Dame Margaret Brimble FRS is the Director of Medicinal Chemistry and a Distinguished Professor at the University of Auckland where her research program focuses on the synthesis of bioactive natural products, antimicrobial peptides, cancer vaccines, glycopeptides, self-assembling peptides and peptidomimetics. She has published >485 papers, 70 reviews and is an inventor on >50 patents. In 2018 she was elected a Fellow of the Royal Society London, awarded the Royal Society of Chemistry George and Christine Sosnovsky Award in Cancer Therapy and conferred the Queens Honour Dame Companion of the New Zealand Order of Merit (DNZM). She won the 2016 Marsden Medal, the 2012 RSNZ Rutherford (NZ’s top science prize), MacDiarmid and Hector Medals, the 2011 Royal Australian Chemical Institute Adrien Albert Award, the 2010 RSC Natural Products Award, the 2007 L’Oreal-UNESCO Women in Science laureate in Materials Science for Asia-Pacific, a 2015 IUPAC Distinguished Women in Chemistry/Chemical Engineering Award. She is an Associate Editor for Organic Letters, Past-Associate Editor for Organic and Biomolecular Chemistry, Past-President of IUPAC Organic and Biomolecular Division III, Past-President of the International Society of Heterocyclic Chemistry and Past-Chair of the Rutherford Foundation RSNZ. She discovered the first drug NNZ2566 named “trofinetide” to treat Rett Syndrome and Fragile X Syndrome that is in phase III clinical trials with Neuren Pharmaceuticals (http://www.neurenpharma.com) and Acadia Pharmaceuticals. A second unique neurotrophic drug candidate NNZ-2591 also discovered by Professor Brimble’s lab has recently been demonstrated to give positive results in pre-clinical models of three additional neurodevelopmental disorders – Angelman syndrome, Pitt Hopkins syndrome and Phelan-McDermid syndrome. Neuren is filing an Investigational New Drug Application (IND) for NNZ2591 with the US Food and Drug Administration and commencing Phase 2 studies in the second half of 2020. Margaret also co-Founded the spin-out company SapVax with US$6 million funding from BioMotiv USA to take self-adjuvanting cancer vaccines based on a novel chemistry platform, to clinical trial (see: https://sapvaxllc.com). She has also entered a licensing and research and development agreement with the New Zealand company Living Cell Technologies (https://www.lctglobal.com) to progress two series of lipopeptide drug candidates to clinical trial for the treatment of obesity and migraine respectively.
Dr. Grootenhuis was Senior Director of Chemistry at Vertex in San Diego. Prior to joining Vertex in 2002, Grootenhuis worked at CombiChem-DuPont in San Diego (1998-2002), and at Organon in the Netherlands (1989-1998). At Vertex, Grootenhuis was research project-leader in the areas of cystic fibrosis and sodium channel blockers. He is co-inventor of several CFTR modulators that entered clinical development including ivacaftor (FDA approved 2012), lumacaftor (FDA approved 2015), tezacaftor (FDA approved 2018), VX-152, VX-440 (phase 2), VX-659, VX-445 (phase 3), and NaV1.7 blocker VX-241 (phase 1).
Grootenhuis received MSc and PhD degrees in chemistry at the Universities of Utrecht and Twente in the Netherlands. Subsequently, he performed post-doctoral studies in computational chemistry at UC San Francisco (1987-1989) under supervision of Prof. Peter Kollman, followed in 1991 by a short sabbatical with Prof. Martin Karplus at Harvard University. He has held part-time professorship positions at the Universities of Groningen, Twente, and the Free University of Amsterdam.
Grootenhuis has published over 100 peer reviewed papers and is inventor of 65 U.S. patents. He received several scientific awards, most recently the 2013 ACS Heroes of Chemistry award and the 2018 IUPAC-Richter Prize in Medicinal Chemistry.
Jeffery W. Kelly is the Lita Annenberg Hazen Professor of Chemistry at The Scripps Research Institute. Kelly discovered the first regulatory-agency-approved drug (tafamidis vyndaqel; Pfizer) that slows the progression of familial amyloid polyneuropathy (a neurodegenerative disease) as well as familial and sporadic TTR cardiomyopathy (a disease leading to heart failure) caused by the aggregation of different sequences of transthyretin. Currently the Lab is focused on the discovery of first-in-class drugs that would slow the progression of more than one neurodegenerative disease by modulating organismal proteostasis and neuroinflammation. The Kelly group also provided some of the first compelling evidence to support the conformational change hypothesis, the notion that conformational changes alone are sufficient for amyloidogenesis, and they discovered the enhanced aromatic sequon, a N-glycosylated reverse turn structure that stabilizes proteins harboring it.
Kelly has published over 350 scientific papers (ISI h-index > 95), was elected to the to the American Academy of Arts and Sciences (2016) and the National Academy of Inventors (2017), and has received several awards, including the E.B. Hershberg Award for Important Discoveries in Medicinally Active Substances (2019), American Institutes of Chemists Chemical Pioneer Award (2017), the Jacob and Louise Gabbay Award in Biotechnology and Medicine (2016), The Royal Society of Chemistry Jeremy Knowles Award (2016), The American Chemical Society Ralph F. Hirschmann Award in Peptide Chemistry (2012), The Biopolymers Murray Goodman Memorial Prize (2012), The Protein Society Emil Thomas Kaiser Award (2011), The American Peptide Society Rao Makineni Lectureship (Award; 2011), The American Peptide Society Vincent du Vigneaud Award (2008), The American Chemical Society Arthur C. Cope Scholar Award (2001), and the Protein Society–Dupont Young Investigator Award (1999).
Patrick M. Woster currently serves as Professor, Chair and SmartState® Endowed Chair in Drug Discovery at the Medical University of South Carolina. Dr. Woster is a native of Omaha, Nebraska; he received a B.S. in Pharmacy in 1978 and a Ph.D. in Medicinal Chemistry in 1987, both from the University of Nebraska Medical Center. He was a postdoctoral associate in Chemistry at Rensselaer Polytechnic Institute and in Medicinal Chemistry at the University of Michigan, mentored by James K. Coward. Dr. Woster joined the Faculty of Pharmacy at Wayne State University in 1988, and rose to the rank of Associate Professor of Pharmaceutical Sciences in 1995, and Full Professor of Pharmaceutical Sciences in 2001. In 2011, he moved to the Medical University of South Carolina, where he was appointed Professor and SmartState® Endowed Chair in Drug Discovery. In 2015 he was appointed Chair of the Department of Drug Discovery and Biomedical Sciences. A strong proponent of the three traditional areas of academia, Woster has been described as "a quintessential medicinal chemist", striving for excellence in the areas of teaching, research and service.
Dr. Woster has conducted research in multiple areas, including the discovery of inhibitors of the polyamine pathway, novel antimalarial, antitrypanosomal and antibacterial agents, a variety of antitumor compounds, chemopreventive agents and epigenetic modulators. He is perhaps best known for the 1996 discovery (in collaboration with David Edwards) of 6,7-dihydroxybergamottin, the constituent in grapefruit juice that inhibits cytochrome P450 in the gut, altering the bioavailability of numerous therapeutic agents. In collaboration with Robert A. Casero, he was also the first to produce small-molecule inhibitors of lysine-specific demethylase 1, the first-discovered histone demethylase, and to show that inhibition of this enzyme promoted the re-expression of tumor suppressor factors. Most recently, he has expanded his work with epigenetic modulators to non-cancer diseases such as sickle cell disease, cardiovascular reperfusion injury and periodontal disease. His research has consistently been supported by NIH, WHO, the Doris Duke Foundation and several other external sources. He has authored more than 135 manuscripts, holds 11 patents and has given numerous invited presentations. Dr. Woster was Chair of the 2009 Polyamine Gordon Research Conference, and Chair of the 2014 National Medicinal Chemistry Symposium. He has served on numerous grant review panels, including more than 40 NIH study sections, is a member of the Editorial Board of the Journal of Medicinal Chemistry, and reviews for more than 50 scientific journals.
With the exception of a 1-year postdoc in a Department of Chemistry, Dr. Woster has spent his entire career employed at a College of Pharmacy. As an educator, Dr. Woster has mentored 19 Ph.D. and 5 M.S. students, 13 postdoctoral associates, and served on 60 dissertation committees. He has also taught biochemistry and medicinal chemistry to countless pharmacy students at UNMC, Wayne State and MUSC. His teaching is held in high regard, as evidenced by 12 teaching excellence awards between 1988 and 2019.
Dr. Woster is a member of the American Chemical Society, the American Association for the Advancement of Science, the American Association for Cancer Research and the Royal Society of Chemistry. He is a Fellow of the American Chemical Society, the Royal Society of Chemistry, the Asian Federation of Medicinal Chemistry, and the American Association for the Advancement of Science. Most notably, he served as an officer for the ACS Division of Medicinal Chemistry for 25 years as Division Secretary and Webmaster, Division Chair and Membership and International Relations Chair. He was a driving force in initiating the on-line presence of the Division of Medicinal Chemistry, and created the Division web page in 1994. He has also been active in the American Association of Colleges of Pharmacy, and served as Secretary and Chair of the Chemistry Section, Chair of the Academic Sections Coordinating Committee and as a member of the Executive Board of Directors (2004-2005).
Obtained a PhD in synthetic medicinal chemistry from the University of Minnesota & did postdoctoral studies in drug metabolism at the University of Texas, Austin
Paul Erhardt obtained a PhD in synthetic medicinal chemistry from the University of Minnesota and did postdoctoral studies in drug metabolism at the University of Texas, Austin. His early career within the private sector began at a small pharma called ‘American Critical Care’ where he discovered esmolol, an ultrashort-acting beta-adrenergic receptor blocking agent. Still saving lives today in emergency situations, esmolol is regarded as the prototype for a class of compounds that later became known as ‘soft drugs.’ Over the years, esmolol’s ab initio design strategy has been used repeatedly by various companies to successfully produce several additional soft drugs marketed for critical care medicine. Paul then moved into big pharma at Berlex Labs where he rose from Section Head to Assistant Director of global drug discovery and preclinical development, including protection of IP for which he became a certified US PTO Patent Agent by self-study prior to passing the bar exams. Paul’s teams generated several clinical candidates that led him to become an advocate for the consideration of ADMET properties during the early stages of drug discovery. He eventually became a leader within this movement by delivering more than 50 invited lectures and offering numerous short-courses about the importance of drug metabolism while on an international lecture circuit that spanned several years. Paul’s career continued at this juncture by his transition from industry to academia. Entering as a tenured professor, he also became Director of the University of Toledo’s Center for Drug Design and Development (UT’s CD3) nearly twenty years ahead of today’s popular trend to establish such core capabilities within an academic base. In addition to receiving several research and teaching awards from UT, Paul achieved the prestigious rank of a Distinguished University Professor. Continuing to engage in outreach, Paul also became active in the IUPAC where he served as President of the Division for Chemistry and Human Health, and subsequently received an IUPAC award for ‘Outstanding Contributions to the Advancement of Worldwide Chemistry.’ Paul has more than 125 publications, 50 US patents and 7 IND submissions. He remains especially gratified by the drugs he has helped place in the clinic, and by the many individuals who have chosen his academic labs to further their own education; namely 3 sabbatical visitors, 17 postdocs from 7 nations, 25 matriculated PhD and MS graduate students, more than 50 undergraduate students including many honors theses, and 6 high school students as part of the CD3’s ‘Lab Shadow’ program.
Swanlund Professor of Chemistry, directs a vigorous research program in medicinal chemistry
Dr. John Katzenellenbogen, Swanlund Professor of Chemistry, directs a vigorous research program in medicinal chemistry that spans synthesis, biochemical, biophysical, structural and cellular analyses, and medical applications, with a particular focus on the action of estrogens in breast cancer and androgens in prostate cancer. He is recognized internationally as pioneer in the development of novel diagnostic and therapeutic agents for the management of hormone-regulated cancers, including the PET imaging agents FES for estrogen receptors in breast cancers and FDHT for androgen receptor in prostate cancers that are widely used in the clinical development of novel anti-hormones. He has also assisted in the development of a PET-based hormone challenge test that images hormone-induced changes in tumor metabolism and other molecular targets that is proving highly predictive of response to endocrine therapies in breast cancer. Through his extensive work elucidating the molecular details of estrogen action in various target tissues, he has designed novel estrogens that are being actively used to elucidate estrogen actions by numerous collaborators, both locally and elsewhere throughout the world. He has been honored as a Member of the American Academy of Arts and Sciences and is the recipient of numerous awards from the American Chemical Society, the Endocrine Society, the Society for Nuclear Medicine, and the International Society for Radiopharmaceutical Sciences.
Retired from Abbott Laboratories as Senior Research Fellow of the Volwiler Society
Dr. Yvonne C. Martin retired from Abbott Laboratories as Senior Research Fellow of the Volwiler Society. She earned a BA in Chemistry and Biology from Carleton College in Minnesota, and completed her PhD in Chemistry at Northwestern University. Dr. Martin pioneered the application of QSAR, computational chemistry, and cheminformatics in the pharmaceutical industry during her 48 year career at Abbott, developing many new tools and methodologies along the way. She was arguably the first person to apply computational approaches in the pharmaceutical industry. She has authored or co- authored over 60 peer-reviewed publications, 40 book chapters, and 20 reviews. She has edited 6 books, authored the book Quantitative Drug Design, and is an inventor on 8 patents. She was a principal developer of the pharmacophore analysis programs DISCO and ALADDIN.
The medicinal chemistry community has been well served by Dr. Martin's efforts. Dr. Martin has been a member of the Medicinal Chemistry Division since 1971, and served as its Treasurer, 1980-1981. She has served on 11 editorial boards (including Journal of Computer Aided Molecular Design and QSAR and Combinatorial Science) and on NIH and NSF study sections. She was one of the founders of the Cheminformatics and QSAR Society (1989) and served as its chair from 2001-2005. Yvonne Martin is the recipient of numerous awards, including the Herman Skolnik Award from the American Chemical Society's Division of Chemical Information (2009), and the ACS Award for Computers in Chemical & Pharmaceutical Research (2017). She was named a fellow of the American Association for the Advancement of Science (1985), and a fellow of the International Union of Pure and Applied Chemistry (2000) .
Emma Parmee is currently Head of the Discovery Chemistry organization at Merck Research Labs. The organization is responsible for the delivery of small molecule drug candidates and includes Medicinal Chemistry, Structural Chemistry, Modeling & Informatics, Chemical Biology, and Screening Capabilities.
Emma moved to Merck’s West Point facility in 2010, assuming the role of Discovery Chemistry Site Lead where she was responsible for chemistry efforts in Neuroscience, HIV, and Bone. In 2013 she was named Head of the Exploratory Chemistry group, focused on the development of small molecule tools and lead series to enable the validation and progression of innovative new targets into the pipeline. And from 2016 to 2018 Emma led the Chemical Capabilities and Screening Group - a cross-functional department designed to bring together critical adjacent capabilities to accelerate innovation in strategy and maximize pipeline impact
Prior to her move to West Point, Emma was located in Rahway where she worked for nearly eighteen years in Cardiometabolic areas and contributed to several projects which demonstrated clinical POC. She was also privileged to work on the DPP-4 inhibitor project and contribute to the discovery of Januvia™ for which she was awarded Thomas Alva Edison Patent Award from the R&D Council of NJ and the SCI Gordon E. Moore Medal for Innovation. She is also the recipient of the 2018 ACS Medicinal Chemistry Division Award. Her work has led to more than forty issued US patents and over fifty publications in peer-reviewed journals.
Emma came to Merck in 1992 after completing a NATO postdoctoral fellowship at MIT under Professor Satoru Masamune. She obtained her D. Phil. Degree in 1990 at the University of Oxford, studying the total synthesis of milbemycin natural products.
Dr. Crooke is founder, chairman, and chief executive officer of Ionis Pharmaceuticals. During his tenure at Ionis, he has led the scientific development of a new platform for drug discovery, antisense technology and engineered the creation of one of the largest and more advanced development pipelines in the biotechnology industry. Early in Dr. Crooke’s career, he led the creation of the first broad anticancer program in the industry at Bristol-Myers, bringing numerous anticancer drugs to the market in the first five years of his career. He then assumed responsibility for worldwide R&D at SmithKline Beckman. Dr. Crooke has received a number of awards, most recently, the American Chemical Society’s E.B. Hershberg Award for Important Discoveries in Medicinally Active Substances, the Lifetime Achievement Award presented by the Oligonucleotide Therapeutics Society and the Scrip Lifetime Achievement Award. Dr. Crooke received his M.D. and Ph.D. degrees and house staff training at Baylor College of Medicine and has been an active scientist throughout his career. He has published more than 475 scientific publications, edited more than 20 books, has numerous patents, and led the development of more than 21 drugs that have been commercialized.
Professor & Head of the Department of Medicinal Chemistry & founding Director of the Institute for ITDD in the University of Minnesota College of Pharmacy
Gunda I. Georg is Professor and Head of the Department of Medicinal Chemistry and the founding Director of the Institute for Therapeutics Discovery and Development (ITDD) in the University of Minnesota College of Pharmacy. She received a BS in pharmacy (1975) and a PhD in medicinal chemistry (1980) from Philipps University in Marburg, Germany with Manfred Haake. She was a postdoctoral fellow in the Department of Chemistry at the University of Ottawa in Canada (1983) with Tony Durst.
After one year at the University of Rhode Island she joined Dale Boger’s group in 1984 as a Research Assistant Professor in the Department of Medicinal Chemistry at the University of Kansas. Her position was converted the same year to a tenured position. At Kansas, she rose through the ranks to hold a University Distinguished Professorship. In 2007, she moved to the University of Minnesota where she occupies the Robert Vince Endowed Chair and the McKnight Presidential Chair in Medicinal Chemistry.
She is the Co-Editor-in-Chief for the Journal of Medicinal Chemistry, which she took over from another Hall of Fame member, Philip Portoghese. She is an AAAS Fellow, a Fellow of the American Chemical Society, and has received the Ernest H. Volwiler Research Achievement Award of the American Association of Colleges of Pharmacy, the Sato Memorial International Award of the Pharmaceutical Society of Japan, the University of Minnesota Academy for Excellence in Health Research, among others. In 2017, she was inducted into the American Chemical Society Medicinal Chemistry Hall of Fame.
Dr. Georg’s work is described in over 220 publications and she holds a number of patents. She has trained more than 100 PhD and post-doctoral students, most of whom have pursued careers in the pharmaceutical industry. At the University of Kansas, she was the PI of a statewide NIH-funded Center for Cancer Experimental Therapeutics (Center of Biomedical Research Excellence) with a focus on supporting and mentoring junior faculty members that was instrumental in the success of the careers of many junior investigators in the state of Kansas.
During her career, she has worked in several areas of medicinal chemistry in a highly collaborative manner with many research groups. She is known for her research on the medicinal chemistry of the anticancer agents paclitaxel, epothilones, cryptophycins, oximidines, triptolide and phenanthropiperidines. She has also published on synthetic organic chemistry, including total synthesis, and methodology development. Therapeutic areas have included cancer, Alzheimer’s disease, antibiotics, epilepsy, and most recently male and female non-hormonal contraception.
She is a co-inventor of the drug, Lusedra®, a water-soluble analogue of the anesthetic propofol, that was marketed by Eisai Pharmaceuticals in 2009. She is also the co-inventor of Minnelide™ an anticancer agent that entered clinical trials in 2013. She was a co-founder of ProQuest Pharmaceuticals, which was involved in the initial development of Lusedra®.
She is actively involved in professional organizations including the American Chemical Society and the AAAS. She has served for many years as grant reviewer on NIH study sections, for the NSF, AAAS, foundations and universities. She is a member of advisory boards for several scientific journals and Co-Editor of “Topics in Medicinal Chemistry.”
Receiving his MA and PhD working on organotin chemistry under the supervision of Ian Fleming
Mike Rowley studied in Cambridge, receiving his MA and PhD working on organotin chemistry under the supervision of Ian Fleming,. He then spent two years as a postdoc with Yoshito Kishi at Harvard University where he completed the total synthesis of Ophiobolin C.
In 1988 he joined Merck Sharp and Dohme at Terlings Park in the UK as a medicinal chemist, where he was involved in various neuroscience projects in the areas of cerebral ischemia, depression, and anxiety. Latterly he was chemistry project leader for a pain project.
In 2000, Mike moved to become responsible for Medicinal Chemistry and DMPK at the Istituto di Ricerche di Biologia Molecolare (IRBM - MSD’s site in Rome), working in the areas of antivirals and cancer. It was during this time that the group in Rome, in close collaboration with the MRL site West Point, discovered raltegravir (Isentress™), the first in class inhibitor of HIV Integrase. This was followed by IRBM’s discoveries of grazoprevir, an HCV protease inhibitor approved in a combination therapy as Zepatier™ for hepatitis C virus infection and of niraparib (Zejula™), a PARP inhibitor used for ovarian cancer.
Following the closure of the IRBM, he joined AstraZeneca in Mölndal, Sweden in the summer of 2009 as Head of Medicinal Chemistry for the Cardiovascular and Gastrointestinal Research Area. Mike led the department’s work in lead generation and optimization, computational chemistry and scale up covering cardiovascular, gastrointestinal, diabetes and obesity projects.
He returned to MSD in early 2012 as Associate Scientific Vice President, based in Luzern in Switzerland. In this role he was responsible for conceiving and implementing scientific strategy for Merck Research Laboratories chemistry globally.
Mike returned to the UK in 2016, and joined Pharmaron in Hoddesdon as Senior Vice President, Drug Discovery Services Europe in early 2017.
He has published over 100 papers and 40 patent applications. Mike is a Fellow of the Royal Society of Chemistry and received the ACS Heroes of Chemistry award in 2013.
Chief Scientific Officer and leads the discovery research and preclinical development efforts in search of an HBV cure
Michael J. Sofia, Ph.D. received his BA in chemistry with honors from Cornell University in 1980. He went onto receive his Ph.D. in organic chemistry at the University of Illinois Urbana-Champaign in 1984 working for Prof. John Katzenellenbogen where he was an NIH Trainee. His thesis work focused on the design, synthesis and study of mechanism based inhibitors of serine proteases. At the University of Illinois, he received the R.C. Fuson Memorial Award for Superior Performance in Graduate Research. In 1984 he joined the laboratory of Prof. Gilbert Stork at Columbia University as an NIH Postdoctoral Fellow and worked on radical cyclization chemistry and vitamin D total synthesis.
Dr. Sofia began his industrial career in 1986 at E.R. Squibb & Sons where he developed inhibitors of squalene synthetase and HMG-CoA reductase for the treatment of atherosclerosis. His work lead to the identification of the first potent substrate-based inhibitor of squalene synthetase.
In 1989 Dr. Sofia joined Eli Lilly & Company as a Research Scientist. He spearheaded work in the area of leukotriene B4 receptor antagonists for the treatment of inflammation associated with asthma and delivered the clinical candidate LY293111 which progressed to phase II clinical trials. For this effort he was awarded the Lilly Discovery Team Award in 1991. Dr. Sofia also led the PLA2 discovery project team during his tenure at Lilly.
In 1993 Dr. Sofia took his first leap into biotech when he joined Transcell Technologies as the founding Director of Chemistry. He eventually was promoted to Vice President of Research. At Transcell Dr. Sofia pioneered the development of carbohydrate-based technologies for combinatorial chemistry and anti-infective drug discovery. This work led to the development of the first library of a complex anti-infective oligosaccharide and the use of monosaccharides as chemical diversity templates.
Subsequently in 1999, Dr. Sofia joined Bristol-Myers Squibb where he became Group Director of New Leads Chemistry. At BMS, Dr. Sofia built a lead discovery chemistry organization and global research capability that supported all research programs and that led to a dramatic improvement in the identification of new chemical matter to initiate lead optimization programs.
Dr. Sofia left BMS in 2005 to join Pharmasset, Inc. as Vice President of Chemistry and was later promoted to Senior Vice President of Chemistry. There he built the companies capability and programs around novel antiviral agents. His work led to multiple clinical candidates including a number of agents targeting the hepatitis C virus (HCV). His work on HCV resulted in the development of the HCV NS5B polymerase inhibitor, sofosbuvir that utilized a novel liver-targeted prodrug strategy. In 2013 sofosbuvir became the first interferon-free HCV cure therapy approved by both the US FDA and the European EMEA and was marketed as Sovaldi®. It quickly became the most successful drug launched in history and was designated by the World Health Organization as an essential medicine. It soon became the backbone of HCV-cure combination therapies and is part of the fixed-dose combination regimens Harvoni®, and Epclusa® and is used in combination with many other HCV targeted agents. Today over 1.2 million individuals have been cured of HCV using sofosbuvir-based therapeutic regimens.
With the acquisition of Pharmasset by Gilead Sciences in 2012, Dr. Sofia remained with Gilead for a period of time as Sr. V.P. of Chemistry but soon founded OnCore Biopharma to search for a cure for hepatitis B (HBV). OnCore Biopharma became Arbutus Biopharma, Inc. where Dr. Sofia is currently the Chief Scientific Officer and leads the discovery research and preclinical development efforts in search of an HBV cure.
Dr. Sofia has authored over 100 publications, 12 book chapters and numerous abstracts and is an inventor on more than 53 US patents and numerous patent applications. He has been an invited speaker at over 75 national and international conferences and universities. Dr. Sofia sits on several non-profit and for profit advisory boards and is a member of the Board of Trustees for the University of the Sciences, Philadelphia PA. He is also on the advisory boards of Chemical & Engineering News, ACS Medicinal Chemistry Letters, and ChemMedChem
For his work in drug discovery, Dr. Sofia is the recipient of numerous awards. These include the 2014 Pennsylvania Bio Scientific Achievement Award, the 2015 Heroes of Chemistry Award of the American Chemical Society, Foreign Policy Magazine’s 2014 Global Thinkers Award, the Economist Magazine’s 2015 Innovation Award in Biosciences, the 2016 IUPAC-Richter Prize in Medicinal Chemistry, the 2016 Lasker-Debakey Award in Clinical Medical Research, the Gertrude Elion Award from the International Society for Antiviral Research and the 2017 University of Illinois LAS Alumni Achievement Award. He was inducted into the ACS Medicinal Chemistry Hall of Fame in 2017.
ACSRC Director & Management Principal Investigator in the Maurice Wilkins Centre of Research Excellence
Bill Denny received his M.Sc. (1st class) in 1967 and his Ph.D. (under the direction of Professor Con Cambie) in 1969, from the University of Auckland. He then went to Oxford University (UK) (1969-1972) on Salter’s and ICI Fellowships, where he was a Junior Research Fellow at Wolfson College and undertook post-doctoral training in the Dyson Perrins Laboratory, working under the direction of Professor Sir Ewart Jones on the microbiological hydroxylation of steroids.
Bill then returned to New Zealand and joined the Auckland Cancer Society Research Centre (ACSRC) at the University of Auckland as a Senior Research Fellow (1972-1979), working on development of the topo II inhibitor amsacrine, which was FDA-approved in 1984 in a collaboration with Parke-Davis. From 1978-1981 he was a visiting professor at the University of California, San Diego, working in Dr David Kearns’ group on NMR studies of drug/DNA binding kinetics. He then returned to the ACSRC as Deputy-Director (1981-1989) and subsequently as Director (1979-present). From 2002-present he has also been a Management Principal Investigator in the Maurice Wilkins Centre of Research Excellence.
In addition to amsacrine, the ACSRC under Bill’s leadership has to date brought a further 12 drugs to clinical trial (dates given), in collaboration with a range of outside partners; topo II inhibitors Asulacrine (Sparta, 1986), DACA (Xenova, 1995); XR-11576 (Xenova, 2001) and MLN-944 (Millenium, 2003); vascular disrupting agent Vadimezan (Novartis, 1999); kinase inhibitors canertinib (Pfizer, 2000) and PWT597 (Pathway, 2011); blood-cleansing anti-viral agent S-303 (Cerus Corp, 2003); hypoxia-activated prodrugs PR-104 (Proacta, 2006) and tarloxotinib (Threshold, 2012); tuberculosis drug TBA-354 (Global Alliance for TB, 2015) and leishmaniasis drug DNDi-690 (DNDi, expected 2017). He has supervised/co-supervised 11 Ph.D. students to successful completion of their degrees.
Bill has served on the editorial boards of a number of scientific journals, including J. Med. Chem. (ACS, 1995-2001 & 2013-present), ACS Med. Chem. Lett. (ACS, 2012-present), Mol. Cancer Ther. (AACR, 2007-present), Oncology Res. (OUP, 2006-present), Exp. Opin. Inv. Drugs (Ashley, 2005-present), Curr. Opin. Oncol. Metab. Drugs (Current Drugs, 2005-present), Anti-Cancer Drugs (LWW, 2007-2009) and Med. Chem. Rev. (Bentham, 2004-2006). He has also served terms as President of the NZ Institute of Chemistry (1995-1977) and as President of the NZ Society for Oncology (1995-1996).
He has been the recipient of a number of awards, including the Rutherford Medal of the Royal Society of NZ (1995), appointment as an Officer of the NZ Order of Merit (Queen’s Birthday Honours List, 2003), the UK Royal Society of Chemistry Adrien Albert Medal (2005), the Australian Chemical Institute Adrien Albert Award (2006), NZ Biotechnologist of the Year Award (NZBio, 2007), the NZ Society for Oncology Commercialisation Award (2012), the University of Auckland Vice-Chancellor’s Commercialisation Medal (2012), and the American Chemical Society Medicinal Chemistry Award (2014).
Bill was a co-founding scientist of the start-up companies Proacta Inc (San Diego, 2001-2014) and Pathway Therapeutics (San Francisco, 2007-2012). He is an author/co-author on 660 publications (including reviews and book chapters) and a co-inventor on 47 issued US patents. In 2011 he was appointed to a Distinguished Professorship at the University of Auckland.
Dr. Manoj Desai began his professional career in the pharmaceutical industry at Pfizer Inc, Central Research Division, Groton, CT (1986-1994) before moving to Chiron Corporation (1994-2003) as Director of medicinal chemistry. In October 2003, he was appointed Vice President of medicinal chemistry at Gilead Sciences. At Pfizer, he was responsible for the medicinal chemistry efforts that lead to the discovery of oral Substance P antagonist CP-99994 which became the basis for the discovery of the new anti-emetics. At Chiron he formulated macrobead technology for the synthesis and screening of compound libraries for high through put screening and directed research efforts for the discovery of kinase inhibitors. His research efforts at Gilead led to the discovery of cobicistat which is one of components of Stribild® that was approved by FDA for the treatment of HIV infection. He is co-inventor on patents of cobicistat and ledipasvir. Cobicistat is a pharmacoehancer devoid of antiviral activity. Cobicistat has been coformulated in four approved therapies for the treatment of HIV: Stribild® and Genvoya® (marketed by Gilead), Prezcobix® (marketed by Johnson & Johnson), Evotaz® (marketed by Bristol-Myers Squibb). Ledipasvir is a part of two-drug regimen in Harvoni® for curing Hepatitis C virus.
Dr. Desai obtained Ph.D. in organic chemistry from the M. S. University of Baroda in 1981 working with Dr. Sukh Dev and then carried out post-doctoral fellowships at Purdue University (Professor Herbert C. Brown, 1981-1983) and at Harvard University (Professor Elias J. Corey, 1983-1986).
He has co-authored more than 60 publications in peer reviewed journals and is an inventor on more than 25 issued patents. Furthermore, Dr. Desai is Editor-in-Chief for Medicinal Chemistry Reviews (renamed from Annual Reports in Medicinal chemistry; 2012-current), and has co-edited Comprehensive Medicinal Chemistry II (volume 7, 2007) and a book titled Successful Strategies for the Discovery of Antiviral Drugs (2013).
George & Winifred Clark Chair Professor of Chemistry in the Department of Chemistry & Biochemistry
Professor Miller received his B.S. in chemistry from North Dakota State University in 1971, and had the pleasure of participating in undergraduate research with Prof. Socretes Peter Pappas. He obtained his Ph.D. in bioorganic chemistry from Cornell University in 1976 under the direction of G. Marc Loudon, was a National Institutes of Health fellow postdoctoral fellow in the laboratory of Prof. Henry Rapoport at the University of California at Berkeley (1975-77). Currently, he is the he George & Winifred Clark Chair Professor of Chemistry in the Department of Chemistry & Biochemistry. He has spent his entire academic career at Notre Dame, starting as an Assistant Professor in 1977. He served as chair of the department from 2002-2005.
The primary interests in Professor Miller's laboratory are in synthetic and bioorganic chemistry. Most effort is directed toward the development of new methodology and its incorporation into the syntheses and study of biologically important compounds. Special emphasis is given to asymmetric syntheses and studies of hydroxamic acid containing microbial iron transport agents (siderophores), amino acids, peptides, b-lactam antibiotics and carbocyclic analogs of antifungal and anticancer nucleosides. Much effort has addressed the syntheses of functionalized b-lactams, the core unit of an important class of antibiotics. The result has been the development of an efficient, and generally applicable, synthetic approach based on a biomimetic N-C4 closure. This process and subsequent chemistry has facilitated the synthesis of several novel antibiotics and b-lactamase inhibitors. The chemical versatility of the methods indicates that a variety of new b-lactams may be synthesized for studying important structure-activity relationships. Studies of acylnitroso cycloadditions by oxidation of hydroxamic acids led to the development of new methods for the asymmetric syntheses of a variety of biologically interesting compounds. Longstanding efforts have been directed toward the syntheses and study of siderophore-antibiotic conjugates (sideromycins) in a program designed to develop iron transport-mediated drug delivery agents, including those with potential microbe-triggered release processes.
Professor Miller has directly mentored 80 graduate students and more than 70 postdoctoral fellows and research associates. His group has collaborated with interdisciplinary research groups around the world, with notable interactions through sabbatical opportunities in Australia, Germany and New Zealand. The combined studies have produced more than 300 scientific publications, numerous patents and presentations at hundreds of scientific meetings and invited lectureships. Research in the Miller group has been consistently supported by the NIH and several industrial grants. Dr. Miller has served on numerous, editorial boards, including Organic Syntheses and review panels and advisory boards.. He is an active consultant for a number of biotechnology and major pharmaceutical companies, having served 37 continuous years as a consultant at Eli Lilly and Co. He is the co-founder of PracticaChem, LLC that subsequently merged with Hsiri Therapeutics, LLC which he co-founded with Notre Dame alumni to develop technologies discovered in his laboratories.
Major support throughout Prof. Miller’s life has been provided by his wife, Patty. They met while undergraduates at North Dakota State University. They are the proud parents of four grown children, Chris, Katie, Joe and Carl, who, with their wonderful spouses have produced 10 grandchildren as of July, 2016.
Independent consultant, working with both biotech and pharma on all aspects of drug discovery
Ann E. Weber, Ph.D., is currently an independent consultant, working with both biotech and pharma on all aspects of drug discovery. She retired in November 2015 from Merck & Co, where she was most recently Vice President, Lead Optimization Chemistry at the Kenilworth, NJ and Boston, MA sites of Merck Research Laboratories (MRL). In this role, she was responsible for the discovery of innovative therapeutic agents across disease areas. She joined MRL in Rahway, NJ as a Senior Research Chemist in 1987.
Dr. Weber’s research interests include the design and synthesis of ligands for G-protein coupled receptors, ion channels and enzymes. Her work has led to over 40 development candidates, including JANUVIA® (sitagliptin), a treatment for patients with Type 2 diabetes (T2DM), JANUMET®, a fixed dose combination of sitagliptin and metformin, and MARIZEV® (omarigliptin), a once-weekly treatment for T2DM that was approved in Japan in September 2015. One additional drug candidate, vibegron for the treatment of overactive bladder, is in late stage clinical trials.
Dr. Weber is the author or co-author of over 80 publications. She is co-inventor on over 35 issued US patents. Her awards include the Robert M. Scarborough Award for Excellence in Medicinal Chemistry (ACS), the Heroes of Chemistry Award (ACS), the Discoverer's Award (PhRMA), recognizing scientists whose work has been of special benefit to humankind, and a Directors’ Award, the highest honor that Merck confers on its employees. She is a 2013 Liberty Science Center Women in STEM Honoree and the recipient of the 2015 Gift of Mentoring Award from the Metro Women Chemists Committee.
Before joining Merck, Dr. Weber obtained her B.S. degree in chemistry summa cum laude from the University of Notre Dame. She earned her Ph.D. degree from Harvard University, studying synthetic organic chemistry in the laboratories of Professor David A. Evans.
Global Head of Chemistry for Infectious Diseases & Discovery Technology with teams in Basel (CH), Cambridge (US) and Emeryville (US)
Juerg Zimmermann started his professional career with an apprenticeship at Ciba-Geigy. In 1981 he received his BSc in chemistry from the Chemical Engineering School Burgdorf. He then moved to ETH Zürich where he received his Ph.D. in Synthetic Organic Chemistry (1988) under the direction of Prof. Dr. D. Seebach. Juerg complemented his academic education by 2 postdoctoral studies with Prof. Dr. A. Beckwith (Australia) and Prof. Dr. R. Lown (Canada). Research topics included computational studies of radicals and ligand-DNA interactions.
In 1991, Juerg joined the Ciba-Geigy Oncology Research team as a medicinal chemist. Pioneering the kinase drug discovery efforts, Juerg synthesized the compound that would ultimately become Gleevec. Recognizing the importance of lead finding chemistry, Juerg established modern combinatorial chemistry and the Synthesis and Chemogenetics group at Novartis. In 2007 he was promoted to the Head of Oncology & Exploratory Chemistry and in 2010 to the Global Head of Discovery Chemistry. Currently Juerg is the Global Head of Chemistry for Infectious Diseases & Discovery Technology with teams in Basel (CH), Cambridge (US) and Emeryville (US).
For his invention of Gleevec and his scientific contributions to drug discovery, Juerg received the Swiss Chemical Society Sandmeyer Prize, the New York Intellectual Law Association Inventor of the Year Award, the American Association for Cancer Research Bruce Cain Memorial Award, the European Federation for Medicinal Chemistry UCB Award for Excellence in Medicinal Chemistry all in 2002, the Society for Medicines Research (UK) SMR Drug Discovery Award and the Novartis Corporate, Distinguished Scientist Award in 2003, the Pharmaceutical Research and PhRMA Discoverers Award Manufacturers of America in 2004, the Thomas Alva Edison Patent Award from the Research and Development Council of New Jersey and the Heroes of Chemistry Award of the American Chemical Society in 2005, European Inventor of the Year Award in 2009. Juerg nominated for the GIST Hall of Fame by the Life Raft Group in 2010 and was given the Distinguished Industrial Investigator Award by the Swiss Chemical Society in 2015.
In his scientific career, Juerg has published 65 papers, >50 patents and provided >60 presentations and lectures at conferences and universities.
Joined Bristol-Myers Squibb where he led teams in the cardiovascular therapeutic area
Nicholas A. Meanwell received his B.Sc. in Special Honors chemistry from the University of Sheffield, Sheffield, England in 1976. In 1979, he earned a Ph.D. degree from the University of Sheffield under the direction of Dr. D. Neville Jones for studies of the application of alkenyl sulfoxides as key intermediates in the synthesis of a series of 9-deoxyprostaglandin and 9-thiaprostaglandin derivatives and the fragrance dihydrojasmone.
From 1979-1982, Dr. Meanwell conducted post-doctoral training under the supervision of Professor Carl R. Johnson at Wayne State University, Detroit, MI, where he devised a general synthetic approach to sulfoximine derivatives via sulfonimidoyl fluorides, completed the synthesis and sulfoximine-mediated resolution of the ginseng constituent β-panasinsene and devised a synthetic approach to a series of cylcopentane-containing natural products including hop ether, cis-jasmone, sarkomycin and known synthetic precursors to 11-deoxy-prostaglandins and PGE2 from a common intermediate.
In 1982, Dr. Meanwell joined Bristol-Myers Squibb where he led teams in the cardiovascular therapeutic area that developed a series of imidazo[4,5-b]quinolin-2-ones as selective phosphodiesterase III inhibitors, potential antithrombotic agents based on blood platelet aggregation inhibition. His team also mapped the non-prostanoid prostacyclin mimetic pharmacophore, defined most effectively by BMY-45778, a potent partial agonist that inhibited blood platelet aggregation induced by a range of activators, and contributed to the design of inhibitors of thrombin.
From 1991 to 1994, Dr. Meanwell contributed to CNS drug discovery efforts, leading the early phase team that explored the potential of Ca2+-dependent potassium channel modulators, a program that ultimately produced the Maxi K ion channel opener flindokalner (MaxiPostTM) which was advanced into Phase III clinical trials for the treatment of stroke.
In 1994, Dr. Meanwell assumed responsibility for antiviral drug discovery chemistry with the objective of establishing programs directed toward the discovery and development of inhibitors of human immunodeficiency virus-1 (HIV-1), hepatitis C virus (HCV) and respiratory viruses, including influenza and respiratory syncytial virus (RSV). From this initiative, a series of RSV fusion inhibitors were characterized as the first small molecules to interfere with the association of the 6 helical peptide bundle that is a critical step in the virus entry process, with BMS-433771 nominated as a clinical candidate.
A series of HIV-1 attachment inhibitors, the first small molecules described to function by interfering with the interaction between virus gp120 and the host cell CD4 receptor, were identified and optimized, with several compounds advanced into clinical trials from which BMS-488043 established clinical proof-of-concept for this mechanism. BMS-663068, a phosphonooxymethyl prodrug of BMS-626529, has successfully completed Phase 2 clinical trials and has entered Phase 3 studies.
In the arena of HCV inhibition, key discoveries to emerge from the group include the NS5A inhibitor daclatasvir (DaklinzaTM), a first-in-class molecule that established this protein as a clinically-relevant target, and the HCV NS3 protease inhibitor asunaprevir (SunvepraTM), which incorporates the cyclopropyl acylsulfonamide moiety that has been widely adopted. The combination of daclatasvir and asunaprevir in a clinical trial conducted in HCV-infected subjects who had failed pegylated interferon/ribavirin therapy established for the first time that an HCV infection could be cured by direct acting antiviral agents in the absence of immune stimulation. The combination of DaklinzaTM and SunvepraTM was approved in Japan in 2014 for the treatment of genotype 1b HCV infection and DaklinzaTM was approved for marketing by the European Medicines Agency in 2014. In addition, beclabuvir, a thumb site inhibitor of HCV NS5B polymerase, has completed Phase 3 trials as a fixed-dose combination therapy with daclatasvir and asunaprevir.
Dr. Meanwell is the author/co-author of over 200 publications, review articles, book chapters and editorials and more than 170 meeting abstracts. He is named as an inventor/co-inventor of more than 110 granted U.S. Patents. Dr. Meanwell has presented over 120 invited lectures at National and International meetings, Universities and Schools on Medicinal Chemistry describing aspects of antiviral drug discovery and development and principles of drug design.
In 2014, Dr. Meanwell was recognized for outstanding research in the area of HIV/AIDS as a co-recipient of a PhRMA Research and Hope Award for Biopharmaceutical Industry Research for the discovery and development of HIV-1 attachment inhibitors. In 2015, Dr. Meanwell received the 2015 Philip S. Portoghese Journal of Medicinal Chemistry/ACS Division of Medicinal Chemistry Joint Lectureship Award. He was named to the American Chemical Society Medicinal Chemistry Hall of Fame in August 2015.
Professor Richard A. Gibbs graduated from Johns Hopkins University in 1983 with a BS in Natural Sciences. Rich obtained his Ph. D. in 1988 from University of California - Riverside for work on Vitamin D analogs and the development of new synthetic methods with Professor Bill Okamura. He was an NSF postdoctoral fellow at Penn State University from 1988-1991, where he performed catalytic antibody research with Professor Steve Benkovic. Rich began his academic career in 1992 in the Department of Pharmaceutical Sciences at Wayne State University. As an Assistant and Associate Professor Rich made seminal contributions to the areas of medicinal and bioorganic chemistry, and the synthesis and mechanistic evaluation of anticancer drugs. Rich continued this research throughout his tenure at Wayne State and at Purdue University, where he moved to in 2001 as a Professor of Medicinal Chemistry and Molecular Pharmacology. He also served as the Associate Dean for Graduate Programs in the College of Pharmacy at Purdue.
Rich’s research was focused on mechanistic and inhibitory studies of protein prenyltransferases and related enzyme targets, and the design and synthesis of chemical probes of protein prenylation. Many key signal transduction proteins are modified by prenylation of a cysteine residue, followed by a specific proteolytic cleavage step and finally methylation. This has led to intense interest in protein-farnesyl transferase (FTase) inhibitors as potential cancer chemotherapeutic agents, and such compounds are currently in human clinical trials. Rich’s laboratory employed chemical biology approaches to address two key questions in the field of protein prenylation. They explored the substrate specificity of FTase, with the goal of developing potential isoprenoid-based inhibitors or modulators of protein prenylation. Secondly, they used synthetic isoprenoid analogues and labeled derivatives as probes of the biological function of protein prenylation. Rich also developed a new stereospecific route to isoprenoids to synthesize novel, specifically substituted analogues of FPP, the isoprenoid substrate of FTase. This program led to the development of a series of potent inhibitors of FTase and farnesol analogues that are potent inhibitors of the growth of certain human tumor cells in vitro.
In one example of this research program, Rich explored the posttranslational modifications of the signaling protein K-Ras, a protein that is modified post-translationally via sequential prenylation, proteolysis, and α-carboxyl methylation reactions. Both prenylation, which is catalyzed by a soluble prenyltransferase, and methylation, which is catalyzed by a membrane-associated isoprenylcysteine carboxyl methyltransferase (Icmt), are key modifications for the proper localization and biological function of K-Ras. Since mutant K-Ras proteins are key drivers in several human cancers, including ~90% of human pancreatic carcinomas, Rich was very interested in developing inhibitors of the human Icmt-dependent methylation of K-Ras as a way to block its activity in tumor cells. In collaboration with Professor Christine Hrycyna, Rich developed a readily-synthesized class of nanomolar human Icmt (hIcmt) inhibitors based on the substrate N-acetyl-farnesyl cysteine. Structure activity relationship studies led to led to a lead compound, sTAB-F3-Diol, which has a Ki of approximately 50 nM against hIcmt. sTAB-F3-Diol also blocked cellular Ras activation, interfered with Ras signaling through Erk, and exhibited nanomolar to low micromolar IC50 values versus pancreatic tumor cells in both 2D and 3D cell culture systems. Further optimization of the biochemical activity and drug-like characteristics of this promising agent resulted in a new molecule with a Ki value of ~25 nM against human Icmt in in vitro enzymatic assays.
Rich’s awards for research include an American Cancer Society Junior Faculty Research Award, the PhRMA Foundation Research Award, the Lions Club Purdue Cancer Center Research Award and the University Faculty Scholar Award from Purdue University, and for his excellence in teaching he was awarded the Instructor of the Year in the College of Pharmacy, and the College of Pharmacy and Allied Health Professions Excellence in Teaching Award at Wayne State. Rich was always very interested in the application of his work to cancer treatment and was awarded a number of patents focused on his designed inhibitors.
Rich’s service to the medicinal chemistry community was truly exemplary. Highlights of this dedicated service include: Chair, Division of Medicinal Chemistry, American Chemical Society (2006); Vice Chair, Division of Medicinal Chemistry, American Chemical Society (2005); Academic Councilor, Division of Medicinal Chemistry, American Chemical Society (2008-2013); Member, Long Range Planning Committee, Division of Medicinal Chemistry, American Chemical Society (2003-2005); Chair, Awards Symposium, 231st National Meeting of American Chemical Society (2006); Chair, Medicinal Chemistry Award Symposium, National Medicinal Chemistry Symposium (2006); Chair and Organizer, Robertson and MEDI Fellowship Awards Symposium (2006); Member, Organizing Committee – First Annual Indiana Medicinal Chemistry Symposium (2010); Member, Organizing Committee – 3rd Frontiers in Medicinal Chemistry Meeting (2013); Editorial Advisory Board Member, Seventh Edition of Burger’s Medicinal Chemistry and Drug Discovery (2007); Program Leader, Medicinal Chemistry Program, Purdue Cancer Center (2006-2013); Chair, PULSe Executive Committee, Purdue University (2010-2012); Co-chair, National ACS meeting in Anaheim "SERMS" Symposium (2004); Co-chair, National ACS meeting in Philadelphia "Pharmacoproteomics" Symposium (2004); Co-chair, National ACS meeting "Druggable Targets in Functional Lipidomics" symposium (2005); and Program Chair of the 2004 Midwest Enzyme Chemistry Conference.
The field of medicinal chemistry lost one of its cherished colleagues when Rich passed away in February of 2014 after a battle with pancreatic cancer. He is survived by his wife Barbara (Schuster) Gibbs.
Professor, department Chair, & the Alfred and Frances Burger Distinguished Professor of Medicinal Chemistry at Virginia Commonwealth University
Dr. Richard A. Glennon obtained his B.S. degree in Pharmacy and M.S. degree in Medicinal Chemistry from Northeastern University, Boston, Massachusetts. After a year in the pharmaceutical industry (Warner-Lambert/Parke Davis) in New Jersey, he went on to obtain his doctoral degree in Medicinal Chemistry from the State University of New York at Buffalo, followed by an ADAMHA (Alcohol, Drug Abuse, Mental Health) postdoctoral fellowship in psychopharmacology with Dr. Peter Gessner at the School of Medicine, SUNY. He was recruited to a faculty position in the Department of Pharmaceutical Chemistry (which he later changed to the Department of Medicinal Chemistry), Virginia Commonwealth University (VCU), as an assistant professor in 1974.
Dr. Glennon is currently professor, department Chair, and the Alfred and Frances Burger Distinguished Professor of Medicinal Chemistry at Virginia Commonwealth University. He has trained >50 graduate students and >50 postdoctoral fellows and visiting scientists (some of the most talented people imaginable), has published >400 articles and book chapters, and holds a number of patents. Although he has long worked in the area of serotonin and on the development of serotonin sub-population selective agonists and antagonists, this work has been intertwined with the role of serotonin (especially 5-HT2A) receptors in the actions of classical hallucinogens and related psychoactive agents. Additional interests include other central receptors (e.g. benzodiazepine, nACh, sigma, imidazoline, dopamine), as well as membrane transporters (e.g. SERT, DAT, NET, OCT) in the actions of abused agents, antidepressants, and antipsychotics. His research has been continuously funded for >40 years by NIH and other governmental agencies.
He is currently a Senior/Associate Editor for the Journal of Medicinal Chemistry and Editor Emeritus of Medicinal Chemistry Research – two journals founded by Dr. Alfred Burger – and is also a member of the editorial board of Burger’s Medicinal Chemistry. Prior awards include the VCU Award of Excellence (in teaching, research, and service), the American Pharmaceutical Association’s Research Achievement Award, the European Federation of Medicinal Chemistry’s Order of the Oak and Tulip Medal, and the joint Journal of Medicinal Chemistry and ACS Medicinal Chemistry Division’s Portoghese Lectureship.
Global Head of Integrated Drug Discovery for Sanofi with groups in Paris, Frankfurt and Waltham, MA
Dr. John Macor earned his B.S. degree from the University of Notre Dame in 1982 doing undergraduate research with Professor Marvin Miller (a 2016 inductee of the MEDI HOF) and earned his Ph.D. degree in organic chemistry at Princeton University with Professor E. C. Taylor (a 2011 inductee of the MEDI HOF) in 1986. Dr. Macor’s career has spanned four different decades and four different pharmaceutical companies with significant contributions in each of them. He began his career at Pfizer (Groton, CT) in 1986 where he was engaged in a variety of CNS drug discovery efforts, moved to Astra Arcus (Rochester, NY) in 1994 focusing on cholinergic drug discovery, and then moved to Bristol-Myers Squibb in 1997 (Princeton, NJ), starting in cardiovascular and moving to neuroscience in 2001 and immunosciences in 2013. He assumed the role as Executive Director of Neuroscience Discovery Chemistry in 2002 (Wallingford, CT), and he was appointed Executive Director of Immunosciences Discovery Chemistry in 2013 (Lawrenceville, NJ). In October 2016, he accepted the role as Global Head of Integrated Drug Discovery for Sanofi with groups in Paris, Frankfurt and Waltham, MA.
Dr. Macor is a co-inventor of Relpax® (eletriptan) and Nurtec® (rimegepant), two anti-migraine agents of different mechanisms. During his time at Pfizer, he also discovered CP-93,129, a literature standard 5-HT1B/1D receptor selective agonist, and (in addition to eletriptan) he invented CP-122,288, a 5-HT1B/1D agonist that help to confirm the vascular mechanism-of-action of the triptans. While at Astra, he was co-inventor of AZD0328, the first brain-penetrant, selective, full agonist for the α7 neuronal nicotinic receptors, which advanced to Phase 2 trials for schizophrenia. At Bristol-Myers Squibb he led teams and was a co-inventor that discovered BMS-346567 (sparsentan, a dual AT1/ETA receptor antagonist presently in Phase 3 clinical trials for focal segmental glomerulosclerosis [FSGS], a rare kidney disease), BMS-708163 (avagecestat, a gamma-secretase inhibitor for Alzheimer’s Disease that demonstrated beta-amyloid lowering in the cerebral spinal fluid of normal healthy volunteers in a Phase 1 clinical study), and BMS-927711 (rimegepant) now marketed by Biohaven as Nurtec®, a potent CGRP receptor antagonist for the treatment of migraine. Dr. Macor and his teams have moved more than a dozen compounds deep into clinical trials, including LX9211 (AAK1 inhibitor, neuropathic pain, presently in Ph 1b by Lexicon) and vizegepant (CGRP antagonist, migraine, presently in Phase 3 by Biohaven). .
Dr. Macor has authored/co-authored over 195 peer-reviewed publications, is an inventor on more than 120 granted US patents, given more than 100 invited lectures, and has over 500 publications, issued US patents, invited lectures and external meeting presentations. His contributions in the syntheses of heterocyclic compounds, intramolecular 1,2,4-triazine Diels-Alder reactions, indole chemistry, and conformation restriction using heterocycles as bioisosteres in medicinal chemistry are widely cited in the literature. He has participated in and led teams in cardiovascular, metabolic, neuroscience, oncology and inflammation projects, indicative of broad expertise, creativity and impact in medicinal chemistry and drug discovery. Dr. Macor chaired the 2002 Gordon Research Conference on Medicinal Chemistry and the 2006 Gordon Research Conference on Heterocyclic Compounds. Dr. Macor served as Editor-in-Chief of Annual Reports in Medicinal Chemistry for Volumes 42 – 46 (2006 – 2011). Dr. Macor was awarded the 2009 Scarborough Award in Medicinal Chemistry for medicinal chemistry accomplishments under the age of 50 and was made an American Society Fellow in 2011. Dr. Macor served as Chair of the Medicinal Chemistry Division (MEDI) of the American Chemical Society in 2015 and served a total of ten years on the Executive Committee of MEDI in various roles. Dr. Macor was awarded the 2014 Alfred Burger Award in Medicinal Chemistry (a National Award from the American Chemical Society) “to recognize outstanding contributions to research in medicinal chemistry,” and was inducted into the Medicinal Chemistry Hall of Fame in August 2014. He was designated as the 2019 Smissman awardee from the MEDI Division of the ACS “given to a living scientist whose research, teaching or service has had a substantial impact on the intellectual and theoretical development of the field of Medicinal Chemistry.” In 2020, he was awarded the IUPAC-Richter Prize in medicinal chemistry “in recognition of his outstanding creative contributions in the field of medicinal chemistry research on drugs for the treatment of migraine.”
has led research groups focused on the design and synthesis of drug candidates directed at Cardiovascular/Metabolic Disease, Inflammatory Diseases, and Alzheimer’s Disease
Dr. Ruth Wexler received her B. A. degree in Chemistry with honors, with a minor in biology from Boston University in 1977, and her Ph.D. degree in Organic Chemistry from the University of Pennsylvania in 1982 under the direction of Professor Amos B. Smith, III. Dr. Wexler started her career at the DuPont Company, as a Research Chemist in the Medicinal Chemistry Section of the Biomedical Products Division. While at the DuPont Experimental Station she was promoted to positions of increasing leadership responsibility and in 1998 was promoted to Executive Director. In 2001, she joined the Bristol-Myers Squibb Company as Executive Director, Discovery Chemistry, (post-acquisition of DuPont Pharmaceuticals Company) and in the fall of 2002, she moved to Hopewell site in New Jersey where she currently heads the medicinal chemistry efforts directed at Cardiovascular Diseases.
During her career, Dr. Wexler has led research groups focused on the design and synthesis of drug candidates directed at Cardiovascular/Metabolic Disease (hypertension, atherosclerosis, thrombosis, heart failure and obesity), Inflammatory Diseases, and Alzheimer’s Disease. Her group has been involved in many innovative advances, most notably in the Cardiovascular area, where their research efforts have resulted in two important marketed Cardiovascular drugs: Cozaar®, an angiotensin II receptor antagonist; the first novel antihypertensive agent in this class, and more recently Eliquis®, a factor Xa inhibitor; a novel anticoagulant. In addition, her team has discovered 18 additional compounds which were selected for clinical evaluation across a wide range of mechanisms of action.
She has been active in both the Medicinal Chemistry Division and Organic Chemistry Division of the American Chemical Society where she served the Medicinal Chemistry Division as a member of Long Range Planning Committee (1996-1999), as a member of the Predoctoral Fellowship program Committee (1998-2001), and as an Industrial Councilor (2003-2005). In addition, she served the Organic Division as a member of the Executive Committee (1997-2000). Her professional activities include serving on NIH Medicinal Chemistry A Study Section (1999-2003).
She was honored in 2004 as one of twelve Outstanding New Jersey Women in Research by the New Jersey Association for Biomedical Research. In 2011, she was a recipient of the Bristol-Myers Squibb Ondetti and Cushman award for her leadership role in the discovery of Eliquis®. She has been selected as the recipient of the 2015 E.B. Hershberg Award for Important Discoveries in Medicinally Active Substances. Ruth has co-authored over 190 peer-reviewed scientific publications and patents, and has contributed several review articles and book chapters largely in the area of cardiovascular research.
The Ian P. Rothwell Distinguished Professor of Chemistry and Medicinal Chemistry & Molecular Pharmacology at Purdue University
Dr. Arun K. Ghosh is the Ian P. Rothwell Distinguished Professor of Chemistry and Medicinal Chemistry & Molecular Pharmacology at Purdue University. He was born in Calcutta, India and obtained his B.S. degree in Chemistry (1979) and his M.S. degree in Chemistry (1981) from the Calcutta University and the Indian Institute of Technology, Kanpur, India respectively. He received his Ph.D. in organic chemistry (1985) from University of Pittsburgh. He was a postdoctoral fellow at Harvard University (1985-1988) where he worked in Professor E. J. Corey’s laboratories. Following his postdoctoral studies, he joined Merck Research laboratories at West Point, Pennsylvania as a medicinal chemist in late 1988. He worked on a number of research areas including inhibitor design against HIV protease and HIV reverse transcriptase. He also worked on the design of alpha 1-adrenergic receptor subtype-selective antagonists for treatment of benign prostate hyperplasia. In summer of 1994, he began his independent academic career as an Assistant Professor at the Department of Chemistry, University of Illinois, Chicago. He became a tenured Associate Professor in 1997 and then Professor of Chemistry, in 1998. In 2005, he moved to Purdue University, West Lafayette, Indiana as a Professor with a joint appointment in the Department of Chemistry and Department of Medicinal Chemistry & Molecular Pharmacology.
Over the years, Professor Ghosh’s research interests have bridged the areas of bioorganic, medicinal and synthetic chemistry. He has made notable contributions in the structure-based design and development of human medicine. Noteworthy is his creative development of Darunavir, the first FDA approved treatment for drug resistant HIV in 2006. Darunavir has now emerged as frontline therapy for HIV/AIDS. His research efforts on Alzheimer’s Disease set the stage for structure-based drug design efforts on beta-secretase inhibitors. His work on natural product syntheses and subsequent biological studies opened up new promise for treatment of resistant cancers. Ghosh’s research efforts in medicinal chemistry have led to the development of numerous conceptual tools for protein-structure-based drug-design, drug optimization and development. These include, backbone binding concept for designing of HIV-1 protease inhibitors to combat drug resistance, introduction of urethanes of stereochemically defined cyclic ethers and cyclic sulfones in drug design, protein-structure-based design of selectivity for beta-secretase inhibitors for Alzheimer’s Disease and design of reversible and irreversible inhibitors against corona virus proteases. His extensive work in synthetic chemistry resulted in chemical syntheses of numerous targets, covering over three dozen or so different structural families, including bioactive targets such as Laulimalide, Peloruside, Doliculide, Zapanolide, Lasanolide, Platensin and Platensomycin and others. He has been active in the determination of biological mechanisms of action of several anticancer natural products and conceptual design of molecular probes for in-depth studies, as well. These agents were isolated in miniscule quantity and in-depth biological studies could not be carried out. His syntheses and subsequent studies led to the discovery that both laulimalide and pelorusides are potent against taxol resistant cell lines, they bind to a novel drug-binding site on tubulin and show a synergistic effect with taxol. More recently, in collaboration with researchers at the NCI, lasonolide was shown to have a novel chromosome condensing ability. His research is also involved in the development of many new synthetic methodologies including asymmetric syn- and anti-selective adol reactions, asymmetric catalytic Diels-Alder, hetero Diel-Alder, Prins cyclization and asymmetric multicomponent reactions where multiple chiral centers are set in a single one-pot operation. His broad medicinal chemistry research efforts continue to improve the design of HIV protease inhibitors for combating drug-resistant-HIV, but also make significant contribution through the design and development of beta-secretase (memapsin 2) inhibitors for treatment of Alzheimer’s disease, and design of cysteine protease inhibitors against severe acute respiratory syndrome (SARS) corona virus proteases. His research efforts also led to the design and synthesis of the first potent beta-secretase inhibitors, and determination of the first X-ray crystal structure of inhibitor-bound beta-secretase-1, development of tools for selectivity design against beta-secretase 2 (memapsin 1) and Cathepsin D and also creation of inhibitors for clinical development.
Arun Ghosh has been awarded the Chemical Research Society of India Medal (2012); MERIT Award, National Institutes of Health (2011); IUPAC-Richter Prize in Medicinal Chemistry (2010); American Chemical Society’s Arthur C. Cope Senior Scholar Award (2010); Jeananne D. and James B. Chaney Research and Scholarship Achievement Award (2010). He received the ACS Robert Scarborough Excellence in Medicinal Chemistry Award (2008) and has received Novartis Chemistry Lectureship (2010-2011). He was elected as a member of American Association for the Advancement of Science (2005). He is on the current editorial advisory boards of numerous organic and medicinal chemistry international journals including ChemMedChem (2010-2013), ACS Medicinal Chemistry Letters (2010-2013), Journal of Medicinal Chemistry (2010-2013), Letters in Drug Design and Discovery (2010-2013), Reports in Organic Chemistry (2010-2013), Future Medicinal Chemistry (2008-2013) and Virus, Adaptation & Treatment (2008-2013). He is one of the scientific founders of Athenagen, Oklahoma City (2002), an Alzheimer’s drug-development company. Other honors include University Scholar, University of Illinois (1998-2001), National MERIT Scholar, Government of India (1976 - 1981). Professor Ghosh is the author of over 245 scientific research publications in leading international journals and over 50 US patents and patent applications in the fields of inhibitors of HIV-1 protease, beta-secretase inhibitors, SARS protease inhibitors and anti-cancer agents. He edited a book entitled, ‘Aspartic Acid Proteases as Therapeutic Targets’ published by Wiley-VCH in 2010.
He is married to his wife, Jody, an emergency physician and lives in West Lafayette, IN with their three children.
Was previously Senior Vice President, Small Molecule Drug Discovery & co-leader of Research for Genentech Research and Early Development (gRED)
Bruce Roth received his BS in Chemistry from St. Joseph’s College in Philadelphia, PA (1976). He then moved to Iowa State University where he received his Ph.D. in Synthetic Organic Chemistry (1981) under the direction of Dr. George A. Kraus. Bruce then underwent postdoctoral training under the direction of Dr. Andrew S. Kende at the University of Rochester where he completed the total synthesis of the insect antifeedant (±)-Ajugarin IV and the anticancer agent (±)-Quadrone.
In 1982, Bruce joined the Atherosclerosis Chemistry Section of the Warner-Lambert/ Parke-Davis Co located in Ann Arbor, MI. As part of a project aimed at discovering inhibitors of cholesterol biosynthesis, Bruce synthesized the compound that would ultimately be marketed as Lipitor®. For his invention of Lipitor®, Bruce received the 1997 Warner-Lambert Chairman’s Distinguished Scientific Achievement Award, the 1999 “Inventor of the Year Award” from the New York Intellectual Property Law Association, the 2003 American Chemical Society Award for Creative Invention, the 2003 Gustavus J. Esselen Award for Chemistry in the Public Interest, sponsored by the North East Region Section of the American Chemical Society, the 2005 Distinguished Achievement Award from Iowa State University and a 2006 Pfizer Global Research and Development Achievement Award. After taking on progressively greater leadership responsibilities at Parke-Davis and Pfizer, Bruce served as Vice President of Chemistry at the Pfizer Global Research and Development, Ann Arbor Laboratories from 2000- 2007. He also served as an adjunct associate professor in the Department of Medicinal Chemistry in the School of Pharmacy of the University of Michigan from 1996-2007.
In May 2007, Bruce joined Genentech Small Discovery as Senior Director of Discovery Chemistry. On August 10, 2008 he was named one of the American Chemical Society Heroes in Chemistry for the Discovery and Development of Lipitor. In 2010, Bruce was promoted to Vice President of Discovery Chemistry.
Dr. Roth is the inventor or co-inventor of 43 issued U.S. patents and the author or co- author of 50 manuscripts, 35 published abstracts, 9 book chapters and review articles and has given more than 20 invited lectures.
Principal Scientist (Emeritus) in the Research Triangle Institute (RTI) in North Carolina
Mansukh C. Wani was born in Nandurbar, Maharashtra, India. He attended grade school in Nandurbar, Maharashtra and graduated in 1943. He then received his bachelor's degree in Chemistry from the University of Bombay in 1947 and his master's degree in Organic Chemistry from the same University in 1950. In 1958, he came to the United States of America and obtained his Ph.D. degree in Chemistry from Indiana University at Bloomington in 1962, followed by a postdoctoral fellowship at the University of Wisconsin at Madison. He joined the Research Triangle Institute (RTI) in North Carolina in 1962, where he currently holds the position of Principal Scientist (Emeritus).
Dr. Wani's main areas of research have included the isolation and characterization of biologically active natural products and synthesis of anticancer and antifertility agents. In the area of natural products research at RTI, he has been involved in the isolation, purification, and characterization of a wide variety of antineoplastic agents including camptothecin and taxol. These extremely important leads have contributed to the development of four prescription drugs (irinotecan and topotecan from camptothecin, and paclitaxel and docetaxel from Taxol), which together accounted for about one-third of the total cancer chemotherapeutic agent market in 2002. In addition to this ongoing work on plant-derived antitumor agents, continuing efforts have also been directed towards the synthesis of potent water-soluble camptothecin analogs. He has published extensively with over 200 publications and 36 patents to his credit. He has been an invited speaker to a number of national and international symposia on taxol and camptothecin.
Dr. Wani is the recipient of many awards, including the Bruce F. Cain Memorial Award given by the American Association for Cancer Research, the City of Medicine Award given by the Greater Durham Chamber of Commerce, and the National Cancer Institute Award of Recognition, the 2000 Charles F. Kettering Prize of the General Motors Cancer Research Foundation, the Ranbaxy Research Award from the Ranbaxy Science Foundation, and the 2003 Distinguished Alumni Award from Indiana University. In August 2002, a plaque commemorating the discovery of Taxol at RTI was unveiled by the Gifford Pinchot National Forest of Washington State, and in April 2003, the American Chemical Society designated the discovery of camptothecin and Taxol at RTI a National Historic Chemical Landmark. In 2005, Dr. Wani received the North Carolina Award in Science from the Governor of North Carolina. In 2008, Dr. Wani received the Paul Ehrlich Magic Bullet Lifetime Achievement Award.
Dr. Nicholas Bodor is a Graduate Research Professor Emeritus (active) at the University of Florida College of Pharmacy, Gainesville. He joined the university in 1979 as Professor and Chairman of the Medicinal Chemistry Department, and was promoted to Graduate Research Professor in 1983. He is the Executive Director of the college’s Center for Drug Discovery, founded by him in 1986. During his tenure at the University of Florida, Dr. Bodor has supervised the training of more than 50 doctoral students and over 100 postdoctoral level research associates and fellows. In February 2000, he took a leave of absence from his academic posts at the University of Florida in order to accept a position as Senior Vice President of Basic Research and Drug Discovery at the IVAX Corporation. Dr. Bodor then served as Chief Scientific Officer of the IVAX Corporation, Managing Director of the IVAX Drug Research Institute, Budapest, Hungary, as well as President of the IVAX Research Institute until October 2005.
Dr. Bodor's main research interests include design of drugs with improved therapeutic index, design of new chemical delivery systems, computer-assisted drug design, drug transport and metabolism, and theoretical and mechanistic organic chemistry. He has published more than 520 research articles, has over 200 patents, and is on the editorial boards of several international scientific journals. An internationally recognized leader in drug discovery, design and delivery, he has introduced revolutionary, general, comprehensive drug design and drug targeting concepts known as retrometabolic drug design approaches. These concepts strategically combine chemical and enzymatic (metabolic) processes to achieve drug targeting and to produce safe drugs and safe environmental chemicals. The two major classes of the retrometabolic drug design concepts contain “chemical drug targeting systems” (CDS) and the “soft drugs” (SD). Each of these large classes contains various subclasses, based on the different design rules. The design concepts incorporated in the soft drug approaches were used by Dr. Bodor to develop a general and comprehensive program, including a computerized expert system which can be used to design all potential and possible metabolites and the corresponding safe active soft drugs or chemical delivery systems. The soft steroid Loteprednol Etabonate, designed by Dr. Bodor, is on the market in the U.S. and other countries. Other drugs designed by him using the retrometabolic concepts are in advanced clinical development. The progress in these various related fields is reviewed biennially at an international series of symposia Dr. Bodor has founded and organizes entitled, The Retrometabolism Based Drug Design and Targeting Conference. The ninth meeting of this series is scheduled for May 2013 in Orlando; in addition to Florida, venues of the previous eight conferences have included Japan, Hungary and Austria.
Dr. Bodor received his B.S./M.S. degree in Organic Chemistry in 1959 at Bolyai University in Transylvania, and his Ph.D. degree in 1965 from the University of Babes-Bolyai, Cluj and the Romanian National Academy of Sciences. He was a Group Leader at the Pharmacochemical Research Institute in Romania until 1968, when he was offered an R. A. Welch Fellowship at the University of Texas in Austin, where he worked in the field of theoretical organic chemistry with Dr. Michael J. S. Dewar, the first Robert A. Welch Research Chair. In 1972 he became a Senior Research Scientist at ALZA Laboratories in Lawrence, Kansas, which later became INTERx Research Corporation, where he was Director of Research, as well as an Adjunct Professor at the University of Kansas until 1978.
Among his many honors, Dr. Bodor is an elected Fellow of the Academy of Pharmaceutical Sciences, American Association of Pharmaceutical Scientists, American Association for the Advancement of Science, and American College of Clinical Pharmacology. He is also an Honorary Member of the Hungarian Chemical Society and the Panhellenic Society of Pharmacists. Among other honors, Dr. Bodor has been named "The 1984 Florida Scientist of the Year" and received the first AAPS Research Achievement Award in Medicinal and Natural Product Chemistry in 1988, as well as the APhA Research Achievement Award in Pharmaceutical and Medicinal Chemistry in 1989. In 1994 he was named the first recipient of the Nagai Foundation Tokyo International Fellowship. He was named by the American Chemical Society as the 1996 recipient of the Leo Friend Award in recognition of his article entitled, "Design of Biologically Safer Chemicals," published in Chemtech, October 1995. He is the first College of Pharmacy faculty member to receive a Professorial Excellence Award, given by the University of Florida in 1996. The AACP selected Dr. Bodor as the recipient of the 1997 Volwiler Research Achievement Award. In April 2000, Dr. Bodor was named the V. Ravi Chandran Professor in Drug Design and Targeting of the UF College of Pharmacy, the first recipient of this endowed professorship. In February 2002, he was elected a Fellow of the World Innovation Foundation. An honorary Doctor of Science degree was conferred upon Dr. Bodor by the University of Florida in 2005. In 2007, the American Association of Pharmaceutical Scientists awarded Dr. Bodor with the Distinguished Pharmaceutical Scientist Award.
In addition to the awards above, Dr. Bodor has received the highest levels of recognition from his home country of Hungary for his scientific achievements and leadership of the Budapest-based Institute for Drug Research. In 1989 he received an honorary Doctor of Science degree from the Technical University of Budapest, and then was awarded the Doctor Honoris Causa degree from the Medical University of Debrecen in 1990. In 1995 he was elected to the Hungarian National Academy of Sciences. Ferenc Madl, President of Hungary, awarded Dr. Bodor the Gold Cross of Merit of the Hungarian Republic in 2004. In 2010 he received the prestigious Fabinyi Prize of the Hungarian Chemical Society, which is given to scientists living outside Hungary whose outstanding scientific accomplishment have contributed to the reputation of the HCS. In August 2010 at the national celebration of Hungary’s over 1000 years statehood and its canonized first king, St. Stephen, Dr. Bodor was awarded at the Hungarian Parliament, the Commander’s Cross of the Order of Merit of the Hungarian Republic, a prestigious award of civil merit.
Dr. Bodor and his wife Sheryl call Miami their primary residence. He founded Bodor Laboratories, Inc. in 2006, and works there with his son Erik and daughter Nicole (who hold PhD/MBA and PhD degrees, respectively, in the relevant fields) to further develop his drug design strategies to the marketplace. His oldest son Miklós (an MD, PhD) is Chairman of the Clinical Pharmacology Department at the Medical University in Debrecen, Hungary.
In 2012 he was named to the ACS Division of Medicinal Chemistry Hall of Fame.
Regents Professor in the Department of Chemistry and Biochemistry at the University of Arizona
Professor Victor J. Hruby is Regents Professor in the Department of Chemistry and Biochemistry at the University of Arizona. Dr. Hruby was born in Valley City, North Dakota and received his B.S. and M.S., with A. William Johnson, at the University of North Dakota. He then went to Cornell University where he received his Ph.D. with A. T. Blomquist, and then was an Instructor at Cornell University Medical College with Vincent duVigneaud, Nobel Laureate. He moved to the University of Arizona in 1968 as an Assistant Professor. He became Associate Professor with Tenure in 1972, Full Professor in 1977 and Regents Professor in 1989.
Professor Hruby’s research has been primarily in the chemistry, conformation-biological activity relationships, and molecular mechanisms of information transduction and of molecular diseases associated with peptide hormones and neurotransmitters and their receptors that modulate health, disease and human behavior. Specific hormones and neurotransmitters of interest include the opioids, the melanotropins, CCK, glucagon, substance P, oxytocin and related compounds and receptors. Specific methods and approaches used in this research include: de novo design of biologically active peptides and peptidomimetics; asymmetric synthesis; design and asymmetric synthesis of novel chi constrained amino acids; computational chemistry; conformational analysis using NMR, X-ray crystallography and other biophysical tools; combinatorial chemistry; conformation-biological activity relationships, especially as they relate to the design of conformationally and topographically constrained peptide, peptidomimetic and peptide mimetic hormone and neurotransmitter agonists and antagonists for exploring the chemical-physical basis for information transduction in biological systems; the design, synthesis and biological evaluation of peptide and peptide mimetic ligands that affect pain, addictions, feeding behaviors, pigmentation, sexual behavior and motivation, glucose homeostasis, cancer and other biological effects; the chemical-physical basis for behavior; the mechanisms of hormone and neurotransmitter action; peptide mimetic design; and the structure-function of G-protein coupled receptors.
The Hruby group has developed new synthetic methodologies for the assembly of multimeric ligands for the detection and treatment of pain, cancer and other diseases; a new approach to design of ligands for disease states involving the concept of overlapping pharmacophores to address several receptors simultaneously in a single small molecular ligand for the treatment of neuropathic pain without tolerance or addiction and which cross the blood-brain-barrier; and a new biophysical method, plasmon waveguide resonance spectroscopy, which allows one for the first time to examine the structures, thermodynamics and kinetics of GPCRs and other integral membrane proteins on interactions with ligands, modulatory proteins, enzymes, parallel and perpendicular to the membrane bilayer independently. Professor Hruby has published over 1000 articles, reviews, chapters, commentaries and editorials and has over 25 patents and patent filings.
Victor Hruby has received numerous awards and honors, including a Guggenheim Fellowship (1984), the Alan E. Pierce Award (now the Merrifield Award) (1993), a Senior Humboldt Fellowship (1999-2000) and the American Chemical Society Arthur C. Cope Scholar Award (2009). He was awarded a Doctor of Science, Honous Causa from the Free University of Brussels (1989) and was named Regents Professor at the University of Arizona (1989). Additional awards include the American Chemical Society Ralph F. Hirschmann Award (2002), The Jacob Javits Neuroscience Award (1987), the NIH MERIT Award (1988), Sommer Award (2003), Arizona Innovator of the Year (2009), and the Goodman Scientific Excellence and Mentorship Award (2011).
In 2012 he was named to the ACS Division of Medicinal Chemistry Hall of Fame.
George D. Behrakis Endowed Chair in Pharmaceutical Biotechnology & Director of the Center for Drug Discovery
Dr. Alexandros Makriyannis joined Northeastern University in 2005 as the George D. Behrakis Endowed Chair in Pharmaceutical Biotechnology and Director of the Center for Drug Discovery. He is also Professor of both Chemistry and Chemical Biology and Pharmaceutical Sciences. Prior to these appointments, he maintained a highly successful research and teaching program in Medicinal Chemistry and Molecular Cell Biology at the University of Connecticut where he was a Distinguished Professor of Medicinal Chemistry and Drug Discovery.
Since the early stages of his career Dr. Makriyannis has been involved in developing novel methods for target-based drug discovery while also being a practitioner of the field by inventing novel compounds as probes or potential medications. Through his highly creative multidisciplinary work encompassing both chemistry and biology, Dr. Makriyannis has been a pioneer in chemical biology even before this designation was coined. More recently, he has developed a novel multidisciplinary approach for studying drug interactions with membrane protein targets which he has named Ligand Assisted Protein Structure. This unique multidisciplinary approach combines the use of covalent ligands molecular biology and mass spectrometry. It has extensive applications in identifying the drug pharmacophores involved in protein target recognition and activation.
Dr. Makriyannis has also been very inventive and highly prolific. Many of his compounds with the characteristic AM designation are among the most popular pharmacological cannabinergic probes used by the scientific community. In parallel, his work in drug discovery has generated proprietary drug candidates selectively targeting direct and indirect pharmacotherapeutic modulation of cannabinoid signaling. His laboratory has thus produced the first CB2 agonists as drug candidates for neuropathic pain, novel successful FAAH inhibitors for neuroprotection and the first CB1 neutral antagonists which are in late preclinical development for the treatment of obesity and metabolic disorders.
Dr. Makriyannis received the 2012 Award in Medicinal Chemistry at the 33rd National Medicinal Chemistry Symposium held at the University of Arizona, Tucson, AZ.
In 2012 he was named to the ACS Division of Medicinal Chemistry Hall of Fame.
Joined WuxiApptec Ltd. to lead their Early Success Sharing Partnerships business unit which will be based in the US
Dr. Joseph Vacca earned his BS in chemistry in 1977 from St. John Fisher College, Rochester, New York, and obtained his Ph.D. degree in Organic Chemistry under Professor Peter T. Lansbury Sr. at the State University of New York at Buffalo (Buffalo, New York).
He joined Merck Research Laboratories in 1981 as a Senior Research Chemist and has contributed to several primary research projects including: the total synthesis of myoinositol polyphosphates; the discovery of orally bioavailable HIV-1 protease inhibitors, thrombin inhibitors, BACE inhibitors, HCV protease inhibitors and the discovery and development of HIV integrase inhibitors. His work on the HIV-1 protease project led to the discovery of Merck’s HIV protease inhibitor CRIXIVAN™ (indinavir sulfate). He led the HIV integrase discovery program and was co-chair of the early development team responsible for the development of the HIV integrase inhibitor Isentress™. He was also the leader of the HCV protease discovery program and early development team chair. Two compounds from this program are currently in advanced clinical studies (vaniprevir and MK-5172).
In late 2007, Dr. Vacca took on the role of Head of Chemistry of the newly formed External Basic Research (EBR) site at Merck and helped to formulate Merck's external research strategy. In 2009 he was named the Basic Research Site Head of the Merck Frosst Research Institute in Montreal, Canada and helped the site's transition to support infectious diseases until the unfortunate site closure at the end of 2010. After that he simultaneously held two positions within the MRL Chemistry organization as Vice President of Chemistry at the Kenilworth, New Jersey site (until Sept. 2011) and was the Global Head of Structural Chemistry until his retirement from Merck in Nov. 2011. Dr. Vacca recently joined WuxiApptec Ltd. to lead their Early Success Sharing Partnerships business unit which will be based in the US.
Dr. Vacca has over 100 publications and patents and is the holder of many awards including a Merck Directors Award given by the Merck board of Directors (1998); PhRMA Discoverers Award (1999); Intellectual Property Owners "National Inventor of the year Award" (1997); European Inventor of the Year (non-EU nation)(2007); ACS "Award for Creative Invention" (1999); and was a named a Merck Research Laboratories Presidential Fellow in 2008. He was named to the American Chemical Society Medicinal Chemistry Hall of Fame in August, 2012.
Joined the Medicinal Chemistry Department of ICI Pharmaceuticals Group in Wilmington, DE
Peter R. Bernstein received a BS in Chemistry with High Distinction from the University of Rochester in 1973, and earned his PhD with Professor Gilbert Stork at Columbia University in 1977. He then served as an Organic Chemistry Fellow in the laboratory of Professor Barry Trost in the Department of Chemistry at the University of Wisconsin, Madison. In 1979, Peter joined the Medicinal Chemistry Department of ICI Pharmaceuticals Group in Wilmington, DE. He worked there 31 years, continuing through its spin-off as Zeneca Pharmaceuticals and through its merger with Astra Pharmaceuticals to form AstraZeneca Pharmaceuticals. Following his retirement in 2010 he established PhaRmaB LLC as a platform for providing consulting and mentoring in drug discovery and development.
Peter has worked at developing treatments to many different diseases, through multiple mechanisms of action, and has had >10 compounds go into clinical development. Early in his career he initiated and worked on ICI’s leukotriene antagonist project. During this effort he co-invented and helped develop Accolate®, the first leukotriene antagonist to be approved in the US. After developing and out- licensing a back-up, ZD3523, he moved onto inhibitors of human neutrophil elastase. Two compounds from those efforts, ZD8321 and ZD0892, entered development. Since then he has worked on or led chemistry teams targeting: neurokinin antagonists, β-estrogen agonists, γ-secretase inhibitors, H3 antagonists, 5-HT1B antagonists and dual NET/DAT reuptake inhibitors. In the area of neurokinin antagonists he led the chemistry teams working on dual NK1/NK2 antagonists for pulmonary disease [ZD6021 and ZD2249] and NK1 antagonists targeted for CNS indications [ZD4974]. Recently, he led the chemistry of, and then was project leader for, the 5-HT1B-antagonist program [AZD3783] and the H3 antagonist program [AZD5213].
Peter is an author on ~190 scientific papers, presentations, and patents. He is very active in the scientific community as speaker, conference organizer, and board member. In 2011, he was an Alternate Councilor for the MEDI Division of the ACS and was on the Editorial (Advisory) Board for Journal of Medicinal Chemistry and Topics in Medicinal Chemistry. He was the Chair of the 2004 Gordon Research Conference on Medicinal Chemistry, served 8 years as Member and Chair of the Carothers Award Committee of the Delaware Section of ACS and 9 years on the Scientific Advisory Board of the Keystone Symposia. At AstraZeneca, in addition to managerial duties, he progressed on the scientific ladder to the position of Senior Principal Scientist.
He was chosen as the “Distinguished Lecturer” for the 2010 AstraZeneca Excellence in Chemistry Award and in 2011 he was named to the ACS Division of Medicinal Chemistry Hall of Fame.
Research professor of medicinal chemistry at the Medical Research Institute, Florida Institute of Technology
Joseph H. Burckhalter was born in Columbia, South Carolina, in 1912. He earned a B.S. in chemistry from the University of South Carolina in 1934 and an M.S. in organic chemistry from the University of Illinois, Urbana, in 1938. In 1942, he received his doctorate in medicinal chemistry at the University of Michigan, where he had been a graduate student of the legendary Frederick Blicke.
Upon earning his doctorate, Burckhalter went to work for Parke Davis & Co. in Detroit, MI. From the pain-relieving drug now Tylenol, he derived Camoquin, a curative agent for the treatment of malaria. Subsequently, Burckhalter went to the University of Kansas College of Pharmacy, where he initiated the school's doctoral program in medicinal chemistry. He also served at the National Defense Medical Center in Taiwan, and as a Fulbright professor in Germany. In 1960, Burckhalter moved to the University of Michigan, where he took over the department chairmanship from his former mentor, Frederick Blicke. He chaired Michigan's program until Albert B. Prescott Professor Emeritus of Medicinal Chemistry Leroy Townsend was recruited, at which point Burckhalter turned over the reins. Burckhalter, who was a professor of medicinal chemistry at the College of Pharmacy from 1960-82, had a distinguished career in biomedical research as a scientist, teacher and administrator dedicated to utilizing medicinal chemistry for the discovery of new drugs, particularly those to treat cancer and infectious diseases. Although Burckhalter retired from the University of Michigan in 1982 at age 70, he continued to be active in scientific research for a number of years. He served as a research professor of medicinal chemistry at the Medical Research Institute, Florida Institute of Technology, where he continued an active interest in drug development in the areas of cancer and virus diseases such as AIDS. He was a recipient of the American Innovator Award from the U.S. Patent and Trademark Office, the Distinguished Alumni Award at the Universities of South Carolina and Illinois, and the Order of the Palmetto, given by the governor of South Carolina. He is listed in "Who's Who in Medicine and Healthcare."
Among his many achievements, Burckhalter was largely responsible for building the interdepartmental graduate programs in medicinal chemistry at both the University of Kansas and the University of Michigan. In collaboration with Robert Seiwald, he made an essential contribution to the identification of antigens through the synthesis of fluorescein isothiocyanate, better known as FITC. This provided the first practical and first patented antibody labeling agent, and the stable, yellow-green-fluorescent compound has become widely used for rapid, accurate, and economic diagnosis of infectious diseases. FITC has played an important role in identifying the cause of AIDS and can be used to distinguish between different strains of streptococci. It has proved infallible in tests for syphilis. FITC and red RITC (rhodamine isothiocyanate) are used together to quickly diagnose leukemia and lymphoma. FITC also paved the way for the development of other labeling procedures, such as radioimmunoassay and enzyme-linked immosorbent assay (ELISA). Although he passed away in 2004, Burckhalter continues to contribute to drug discovery. The University of Kansas high-throughput screening laboratory maintains a very valuable collection of more than 15,000 unique natural compounds, including a set of information rich molecules developed years ago through the intuition and experience of world-class medicinal chemist Joseph Burckhalter.
Gertrude Elion was born in New York City. She entered Hunter College at the age of 15 and graduated summa cum laude with a BS in chemistry in 1937, when she was only 19. In her first years after college, Elion had difficulty finding work as a chemist. There were few women working in the field, and many laboratories refused to hire women altogether. She acquired experience working in part-time and temporary jobs. While working, she earned an M.S. in chemistry from New York University. She taught high school for a few years, until the Second World War created more opportunities for women in industry.
Hired by Burroughs-Wellcome in 1944, she embarked on a 40-year scientific partnership with Dr. George Hitchings. They set themselves an unorthodox course, attempting to create new medicines by studying the chemical composition of disease cells. Within a few years, this approach had borne fruit with the development of the first two successful drugs for the treatment of acute leukemia: Purinethol and Thioguanine.
Elion's responsibilities expanded, and she began to lead larger and larger teams of her own, discovering compounds such as allopurinol, used for the treatment of gout and to relieve the side effects of chemotherapy. Her discovery of azathioprine, which suppresses the immune system's rejection of foreign tissue made kidney transplants between unrelated donors possible. More than half a million people worldwide have benefited from this discovery since 1963.
In 1967, she was named Head of the Department of Experimental Therapy at Burroughs-Wellcome. Over the following decade, Elion's team at Burroughs-Wellcome entered a field which pharmaceutical companies had previously shunned. They attempted to create compounds which would block viral infections. It was widely believed that any compound capable of suppressing viral activity would be hopelessly toxic. Elion's patience was rewarded with the creation of acyclovir, the world's first successful anti-viral medication. It is often used in the treatment of herpes.
Gertrude Elion officially retired in 1983, but remained active in the scientific world, as a consultant with her old firm, now known as Glaxo-Wellcome, and as an advisor to the World Health Organization and the American Association for Cancer Research. Her name appears on 45 patents.
In 1988, she shared the Nobel Prize in Medicine with her old colleague George Hitchings and researcher Sir James Black. She was one of only ten women to win a Nobel Prize in the sciences, and one of the very few recipients to earn a science Nobel without a doctorate. In 1991, she became the first woman to be inducted into the national Inventor's Hall of Fame, and was presented with the National Medal of Science by President George Bush.
Research Chemist at Pfizer’s Medical Research Laboratories in Groton, Connecticut
Hans-Jürgen Hess received his Ph.D. in organic chemistry in 1957, working with Professor Hans Herloff Inhoffen at the Technical University Braunschweig, Germany. After postdoctoral work with Professor Randolph T. Major at the University of Virginia and Professor E.J. Corey at the University of Illinois, he joined Pfizer’s Medical Research Laboratories in Groton, Connecticut, as a Research Chemist in 1959. Hans Hess has a distinguished record in drug discovery and development. He was responsible for all Pfizer Medicinal Chemistry Research and affiliated functions in the US and Japan during a period of steady internal growth and productivity.
In 1963, he conceived and implemented a program for the discovery of a peripherally acting antihypertensive agent, work that culminated in the discovery of prazosin (Minipress®). At the time of its US introduction in 1976, Minipress® was a major advance in the treatment of mild to moderate hypertension and was mechanistically distinguished from any other antihypertensive agent. As a selective α1-adrenergic blocker, it was free of unfavorable effects on blood lipid profiles of other types of antihypertensive drugs in use. In 1988, Minipress® ranked third in the worldwide antihypertensive market. The drug was also shown effective in the treatment of BPH (benign prostatic hyperplasia), and is the prototype of a class of structural analogs (doxazosin, terazosin, alfuzosin) developed and marketed for this indication. Prazosin became the laboratory standard in adrenergic receptor research and was the key to the α1-subclassification of adrenergic receptors. In 1991, Hans Hess received the Pharmaceutical Manufacturers Association (PMA) Discovery Award for the discovery of prazosin.
Hans Hess’s research interests and expertise range over a wide area of medicinal chemistry. He led the discovery efforts resulting in pirbuterol (Maxair®), a tissue selective ß-adrenergic agonist bronchodilator, sulprostone (Nalador®), a tissue selective prostaglandin analog for obstetric and gynecological uses, and the first potent, non-peptidic neurokinin-1 (substance P) antagonist. In parallel with his responsibilities in the US, he established in 1983 fully integrated Pfizer drug discovery operations in Japan, involving medicinal chemistry, pharmacology, biochemistry, molecular biology, drug metabolism, state-of-the-art microbial natural product screening and structure determination, and development functions. Building on the experience of automating microbial natural product screening in Japan, he subsequently established high throughput screening (HTS) of chemical compound libraries in receptor, enzyme, and cellular assays, Pfizer being one of the first companies in the industry implementing this technology for lead discovery. Hans Hess’s achievements have been chronicled in about 100 issued US patents and 70 publications and abstracts.
Throughout his scientific career, Hans has been actively involved in professional activities contributing to the advancement of Medicinal Chemistry in numerous ways. For 5 years, from 1979-1983, he was Editor-in-Chief of “Annual Reports in Medicinal Chemistry”. He was Chairman of the Medicinal Chemistry Gordon Research Conference in 1986, and served on Awards Nominating and Long-Range Planning Committees of the Division of Medicinal Chemistry.
Hans Hess retired from Pfizer in 1996 after more than 36 years involvement in drug research. Since then he has been a member of Scientific Advisory Boards and serving as a consultant of a number of pharmaceutical companies.
Internationally renowned medicinal chemist & expert in drug design & drug discovery
M. Ross Johnson, Ph.D. is an internationally renowned medicinal chemist and expert in drug design and drug discovery who has had a long and productive career as an inventor, discoverer, executive and entrepreneur in the Pharmaceutical and Biotech industries. His extensive contributions to drug discovery and development and basic science have resulted in over 300 scientific publications, patents, and invited presentations which include 131 issued U. S. Patents and three landmark primary research publications averaging over a thousand citations each. Dr. Johnson is widely known for his discovery of nonclassical cannabinoid analgesics exemplified by levonantradol (U.S. Patent 4,486,609), CP-55,940 (U.S. Patent 4,340,737) and CP-55,244 (U.S. Patent 4,306,097). His extensive research resulting in the medicinal chemical conceptualization, biochemical characterization, and the neuroanatomical localization of the cannabinoid receptor led to the identification of this hypothesized receptor in rodent, primate and human brains. He is also a discoverer and an inventor of record of the ultra short acting analgesic/anesthetic remifentanil /ULTIVA® (U.S. Patent 5,019,583), the oral anti-diabetic englitazone (U.S. Patent 4,739,079), the prostaglandin analog sulprostone/Nalador® (U.S Patent 4,244,887), the use of viral membrane fusion inhibitors such as enfuvirtide (Fuzeon®) in combination with other retroviral drugs (U.S. Patent 6,475,491) to reduce HIV viral load, and the recent discovery of novel epithelial sodium channel blockers such as Parion Sciences 552 and Gilead Sciences 9411 (U.S. Patent 6,858,615). These latter agents are being developed for the treatment of cystic fibrosis and chronic bronchitis, the treatment of xerostomia caused by Sjögren’s disease, and as a medical countermeasure therapy to treat victims and protect first responders against threats involving airborne radioactive particles and bioterrorism agents such as anthrax and plague.
Dr. Johnson is currently Chief Executive Officer, Director and Co-Founder of Parion Sciences, Inc. From 1995-1999 he was President, Chief Executive Officer and Chief Scientific Officer of Trimeris, Inc. (TRMS), a company he took public in 1997. From 1987 -1994 he was Vice President of Chemistry at Glaxo Inc. (GSK) where he was part of the original scientific founding team for Glaxo's research entry in the United States. Prior to 1987 Dr. Johnson served in key scientific and research management positions with Pfizer Central Research (PFE) from 1971-1987. Ross Johnson received his B.S. degree in Chemistry from the University of California at Berkeley in 1967 and a Ph.D. degree in organic chemistry from the University of California at Santa Barbara in 1970.
Dr. Johnson has served, with distinction, as Chairman of the Organic Chemistry Division of the American Chemical Society and Chairman of the Gordon Research Conference on Natural Products and is a founder of both the International Cannabinoid Study Group and the Glaxo-UNC Frontiers in Chemistry and Medicine Symposia. His contributions to medicinal chemistry have been recognized by his appointment as Adjunct Professor of Chemistry at a number of universities, most recently at the University of North Carolina at Chapel Hill. He currently serves on the Advisory Boards of the College of Chemistry at the University of California at Berkley, the Department of Chemistry at the University of North Carolina at Chapel Hill, the Biomanufacturing Research Institute and Technology Enterprise (BRITE) Center for Excellence located at North Carolina Central University, the Eshelman School of Pharmacy at the University of North Carolina at Chapel Hill and the Graduate Education Advisory Board at the University of North Carolina at Chapel Hill.
In 1989, as recognition for his contributions and influence in solving problems of mutual interest in government, academia and industry, Ross Johnson was named the first ever "Distinguished Research Fellow" in the Laboratory of Medicinal Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health. He was an elected member of the Steering Committee of the Drug Discovery Management Section of the Pharmaceutical Manufacturer's Association and has served on the Executive Committee of the American Chemical Society's Campaign for Chemistry.
Dr. Johnson has served on numerous corporate and not for profit boards and currently holds corporate board positions with Cortex Pharmaceuticals (COR) and Parion Sciences. He has also served on the following Boards: Delta Pharmaceuticals, Hesed Biomed, Kainos Medicine, Inc, Trimeris Inc., Parnasus Pharmaceuticals, The Executive Committee of the Organic Chemistry Division of the American Chemical Society, The College on the Problems of Drug Dependence, the Inter-Company Collaboration for AIDS, the North Carolina State University Board of Visitors, the Board of Governors of Research Triangle Institute and the Child and Family Agency of Southeastern Connecticut. He has also served as a Special Advisor to Nobex, Ceretec, Athrogenics (AGIX) and Albany Molecular (AMRI). He is a reviewer of scientific papers for several major research publications and has served on the Editorial Advisory Boards of the Journal of Medicinal Chemistry and the Journal of Drug Development Research.
He and his lovely wife, Charlotte, live in Chapel Hill, North Carolina and have two sons, Michael and Gregory. Michael is a sales professional and resides in Henderson, North Carolina with his wife Andie. Gregory is a chef and resides in Napa Valley, California with his wife Teresa. Ross and Charlotte have six amazing and wonderful grandchildren-Mack, Macy Lee, Sophia, Becca, Lottie and Ella Cate.
Professor at the University of Kansas & Chair of the Department of Medicinal Chemistry
Mathias P. Mertes was born in Chicago on April 22, 1932. He was raised in Chicago and prepared early for a career in pharmacy, having delivered prescription drugs on his bicycle for his father's neighborhood pharmacy. He received a B.S. degree in pharmacy from the University of Illinois in 1954. Because of a keen interest in research he entered graduate school at the University of Texas, where he received an M.S. degree in medicinal chemistry with C. O. Wilson in 1956. He subsequently earned a Ph.D. degree with Ole Gisvold from the University of Minnesota in 1960. Upon completion of his Ph.D., Matt accepted a position at the University of Kansas as an assistant professor of medicinal chemistry. There he joined Ed Smissman, who had just moved to Kansas as Chair of medicinal chemistry, and who had been an undergraduate instructor of Matt's at the University of Illinois. Matt advanced rapidly in his career, reaching the rank of Professor in 1968. Together, Matt and Ed Smissman built a strong and vigorous department and established many traditions that still persist to this day. Matt continued this legacy after Ed's death in 1974, serving as Chair of the Department of Medicinal Chemistry from 1974-1975.
As a teacher Matt was extremely dedicated, being popular with graduate and undergraduate students alike. He won several teaching awards, including the University of Kansas EXXON Award in 1986 and the Rho Chi Teaching Award presented by students of the School of Pharmacy. Matt was also a finalist for the prestigious H.O.P.E. (Honor for the Outstanding Progressive Educator) Award, an award given annually by the University's senior class. He was also one of the pioneers in advocating and providing continuing education for practicing pharmacists in Kansas, participating with great enthusiasm in continuing education seminar trips around the state. He was also one of the founders of the highly successful medicinal chemistry meeting-in-miniature known affectionately as the MIKI meeting. Since 1963, this meeting has been held annually on a rotating basis among the Universities of Minnesota, Iowa, Kansas, and Illinois.
As a research scholar Matt's interests varied widely. They included: 1) development of methodology for the synthesis of nucleoside, nucleotide, and nucleic acid analogs, 2) studies on thymidylate synthetase model systems and reaction mechanisms including the design and synthesis of thymidylate synthetase inhibitors, 3) the design, synthesis and evaluation of glutamate receptor probes that discriminate between glutamate receptor subtypes, and 4) with his wife, Kristin, University Distinguished Professor of Chemistry at the University of Kansas, polyammonium macrocycle synthesis, ligand complexation, and mechanism of catalysis of formyl phosphate and ATP hydrolysis. Matt received an NIH Career Development Award (1967-72) enabling him to spend one year in the laboratory of F. Sorm at the Czechoslovakian Academy of Sciences in Prague (nucleic acid chemistry). He also spent six months at the University of Colorado studying in vitro mRNA translation. In 1983, he and Kristin spent a sabbatical in the laboratory of 1987 Nobel laureate Jean-Marie Lehn at Strasbourg. During his career Matt published over 100 scientific papers and directed 23 graduate students to the Ph.D. degree, in addition to training five M.S. students and a number of postdocs. Matt served as Chair of the Division of Medicinal Chemistry of the American Chemical Society in 1978, as Vice-chair in 1977, and served on the Division's membership, long-range planning and membership directory committees. He also served on the editorial boards of the Journal of Medicinal Chemistry and Nucleosides and Nucleotides. His service also included a four-year term on the Medicinal Chemistry A Study Section at NIH and another four-year term on the NIH Biomedical Research Support Committee.
After Matt's untimely death from a heart attack on Thursday, April 6, 1989, Frances Degan Horowitz, Vice Chancellor for Research and Graduate Studies at Kansas, remarked, "He was always available to help on projects that transcended his lab, his department, his school and his adopted state. He did all this with personal grace, with uncommon gentleness and with generous spirit. Such personal qualities ensure that our memories of an exceptional friend and colleague will remain vivid, inspiring and enduring."
The Mathias P. Mertes Memorial Fund was established by the University of Kansas Endowment Association with contributions from his family, friends, colleagues, students and co-workers to memorialize Matt's dedication to excellence in research and scholarship through a student-initiated lecture series.
Used with permission of the University of Kansas Department of Medicinal Chemistry.
A. Barton Hepburn Professor of Organic Chemistry & Organic Chemistry Emeritus. Senior Research Chemist at Princeton
Prof. Edward C. Taylor was born in Springfield, Massachusetts, on August 3, 1923. He received both his B.A. (1946) and his Ph.D. (1949) degrees from Cornell University. He was a Merck Postdoctoral Fellow (1949-50) of the National Academy of Sciences in Zürich, Switzerland, where he studied with Leopold Ruzicka, and then the du Pont Postdoctoral Fellow at the University of Illinois (1950-51). He joined the faculty at the University of Illinois in 1951, and then moved to Princeton University in 1954. In 1966 he was appointed A. Barton Hepburn Professor of Organic Chemistry, a position he held until July, 1997, when he was appointed A. Barton Hepburn Professor of Organic Chemistry Emeritus and Senior Research Chemist at Princeton. He served as Chairman of the department from 1973 until 1979. He was awarded the degree of Hon. D.Sc. from Hamilton College in 1968, the Distinguished Hamilton Award in 1978, and the Hamilton Distinguished Alumni Award in the fall of 1990. He received an honorary D. Sc. degree from Princeton University in 2010.
Taylor was an NSF Senior Faculty Fellow at Harvard University, Distinguished Visiting Professor at the University of Buffalo; Visiting Professor at the Technische Hochschule, Stuttgart, the University of East Anglia, Norwich, the University of Freiburg, and the Weizmann Institute; and Backer Lecturer at the University of Groningen. He is a former member of the Chemistry Advisory Committee of the Cancer Chemotherapy National Service Center, of the Air Force Office of Scientific Research, and of the Board of Editors of the Journal of Medicinal Chemistry and the Journal of Organic Chemistry; he is currently a member of the Board of Editors of Synthetic Communications, Heterocycles, Pteridines, and Advances in Heterocyclic Chemistry. He served as Chairman of the Organic Division of the American Chemical Society in 1976-77, and is currently Chair of the Scientific Advisory Board, Privileged Discovery Partners, PDP.
Other honors include Fulbright, Guggenheim and Alexander von Humboldt awards, the 1974 American Chemical Society Award for Creative Work in Synthetic Organic Chemistry (for his work in organothallium, heterocyclic, pteridine and folate chemistry), the 5th International Award in Heterocyclic Chemistry, the Gowland Hopkins Medal in 1993, and the 1994 Arthur C. Cope Scholar Award of the American Chemical Society. He was the recipient of the 2004 Thomas Alva Edison Award for Invention for his patent on the compound that became Alimta, a new and broadly effective anticancer drug developed and marketed by Eli Lilly and Co, and was selected for the 2006 Heroes of Chemistry Award, together with two scientists from Eli Lilly and Co., and again by the American Chemical Society, for his work on the discovery and development of Alimta “that has led to the welfare and progress of humanity”. By end of 2010, Alimta stood as the most successful new cancer drug, based on sales, in the history of the pharmaceutical industry. He was inducted into the New Jersey Inventors Hall of Fame in 2009, received from the American Chemical Society the Alfred Burger Award in Medicinal Chemistry in March, 2010, and was inducted into the Medicinal Chemistry Hall of Fame of the ACS in 2011.
For the past fifty-five years Taylor has been consultant for the research divisions of a number of pharmaceutical and chemical companies. He also serves as editorial advisor in the field of organic chemistry to John Wiley & Sons. He is a member of the ACS, The Royal Society of Chemistry, the German Chemical Society, Phi Beta Kappa, Phi Kappa Phi, and Sigma Xi, and is a Fellow of the American Institute of Chemists, the New York Academy of Sciences, and the AAAS.
In 1968 he joined Dr. Arnold Weissberger as co-editor of the Wiley-Interscience series The Chemistry of Heterocyclic Compounds (Taylor was the sole editor since Dr. Weissberger's death in 1984; Professor Peter Wipf joined him as coeditor in 1998), and of the series General Heterocyclic Chemistry. Thus far 79 volumes have been published under his editorship. He has produced a 24-hour Film Course on Principles of Heterocyclic Chemistry, and a companion Audio Course, both distributed by the American Chemical Society; these were followed by an extensive lecture course aimed at industrial research laboratories on Utilization of Heterocycles in Organic Synthesis. He is also the editor of Advances in Organic Chemistry (9 volumes to date) and was co-editor with Pfleiderer of Pteridine Chemistry (1964), co-author (with Alexander McKillop) of The Chemistry of Enaminonitriles and o-Aminonitriles (1970), and author of two books on Principles of Heterocyclic Chemistry.
Prof. Taylor is the author of over 450 scientific papers and 52 U.S. patents on heterocyclic chemistry, organothallium chemistry, natural product chemistry, medicinal chemistry and synthetic methodology.
Professor and chair of the Department of Pharmaceutical Chemistry in the UCSF School of Pharmacy
James A. Wells, PhD, focuses on development of enabling technologies for engineering proteins and for identifying small molecules to aid in drug discovery. He is interested in the discovery and design of small molecules and enzymes that trigger or modulate cellular processes in inflammation and cancer. Using small molecules and engineered proteins, the Wells lab is studying how enzymes known as proteases are turned on to cleave particular proteins in cells. The lab is currently focusing on a set of proteases, known as caspases, responsible for fate determining cellular decisions involved in apoptosis and innate inflammation among others. These enzymes act as cellular remodelers and help us understand the essential protein structures that support life.
Wells is a professor and chair of the Department of Pharmaceutical Chemistry in the UCSF School of Pharmacy. He holds a combined appointment as professor in the Department of Cellular & Molecular Pharmacology in the School of Medicine. He joined UCSF in 2005 as holder of the Harry Wm. and Diana V. Hind Distinguished Professorship in Pharmaceutical Sciences. Wells also founded and directs the Small Molecule Discovery Center (SMDC) located at UCSF’s Mission Bay campus. He earned a PhD degree in biochemistry from Washington State University with Professor Ralph Yount in 1979 and completed postdoctoral work at Stanford University School of Medicine with Professor George Stark in 1982. Before joining UCSF, Wells was the founding scientist in Genentech’s Protein Engineering Department, and in 1998 Wells co-founded Sunesis Pharmaceuticals.
Wells is a recipient of the Hans Neurath Award by the Protein Society, the Pfizer Award and Smissman Award given by the American Chemical Society, the Perlman Lecture Award given by the ACS Biotechnology Division, the du Vigneaud Award given by the American Peptide Society, the Merck Award from the ASBMB and in 1999 a member of the National Academy of Sciences.
Alfred and Francis Burger Emeritus Professor of Medicinal Chemistry & Biological Chemistry, & Emeritus Director of the Institute for Structural Biology and Drug Discovery at Virginia Commonwealth University
Dr. Donald J. Abraham is the Alfred and Francis Burger Emeritus Professor of Medicinal Chemistry and Biological Chemistry, and Emeritus Director of the Institute for Structural Biology and Drug Discovery at Virginia Commonwealth University. Prof. Abraham received his BS degree in Chemistry from Penn State University (1958), an MS in Chemistry at Marshall University (1959) and his Ph.D. degree at Purdue (1963). Following the completion of his degree, he completed postdoctoral studies with Prof. Alfred Burger at the University of Virginia. He joined the faculty in the Department of Medicinal Chemistry at the University of Pittsburgh in 1964, and rapidly rose through the ranks, becoming a full professor in 1972. Don assumed the chairmanship of the department in 1969, and served in that capacity until 1988. In that year, Don was appointed chair of the Department of Medicinal Chemistry at Virginia Commonwealth University, a position he held until 2007. During his academic career, Don held affiliate appointments in several departments, including physics, crystallography, psychiatry, pharmacology, biomedical engineering and biophysics; these appointments are a testament to his versatility and breadth of expertise in science, and to the interdisciplinary nature of his drug discovery research.
Prof. Abraham has conducted research in a variety of therapeutic areas, but he is perhaps best known as a pioneer in the area of structure-based design. His studies of the structure of hemoglobin and the use of that structure to design specific allosteric ligands represent seminal advances in computer-based drug design. He is recognized as the first medicinal chemist who applied protein crystallography to drug design, after proposing this concept to Alfred Burger in 1963. He presented a paper at the Alfred Burger retirement symposium that is regarded as the first reported use of crystallography in medicinal chemistry. Working with Peter Goodford from Wellcome UK and Nobel laureate Max Perutz, Don applied structure-based design methodologies to discover novel allosteric modulators of hemoglobin function. He published a landmark paper in the Proceedings of the National Academy of Science U.S.A. (1983) that describes the first successful use of fragment-based drug design. His efforts ultimately resulted in the discovery of a hemoglobin allosteric effector, RSR-13, that was advanced to human clinical trials for hypoxic disease. Another analogue resulting from this work, 5-HMF, is currently in a phase 1 trial jointly administered by NIH and AesRX Inc.
During his career, Don founded or co-founded three successful companies: Allos Therapeutics, which produced an FDA-approved anticancer drug, eduSoft, a software company that markets the structure-based design program HINT, and kSERO that specializes in teaching children science through game playing. He also founded and was the first director of the Institute of Structural Biology and Drug Discovery at the Virginia Commonwealth University. This has been acknowledged as the first such institute in academia. In addition to these achievements, he has provided outstanding service to the field of medicinal chemistry, including serving as chair of the National Medicinal Chemistry Symposium, a member of numerous NIH study sections and as chair of the ACS Division of Medicinal Chemistry. Don has published more than 175 peer-reviewed articles, has been awarded $12.5 million in external funding, and has 35 awarded or pending patents. Notably, Don edited the 6th Edition of Burger's Medicinal Chemistry, and co-edited the 7th Edition of that series. He is the recipient of numerous awards and accolades, including the Humboldt Prize (1973), the Virginia Outstanding Scientists of the Year (2001), the Amgen Paul Dawson award in Biotechnology (2002), an honorary doctorate from the University of Parma (2005) and many others. He is also an elected Fellow of AAAS.
Dr. Choung Un Kim was born in Tokyo, Japan in 1942. He became the first member of his family to go to college, attending the University of Tokyo in 1961, where he earned a Bachelor of Science degree in Pharmaceutical Sciences and a Master of Science degree in Organic Chemistry. He then emigrated to the United States in 1967 and obtained a PhD in Organic Chemistry at the University of Oregon by 1970. He then worked under Professor EJ Corey as a Post Doctoral Fellow at Harvard University, where they discovered the Corey-Kim oxidation reaction, which is used to synthesize aldehydes and ketones from primary and secondary alcohols.
Dr. Kim then went to work for Bristol-Myers for 21 years before joining Gilead Sciences in 1994. There he made his most important discovery, Oseltamivir (Tamiflu®), which has subsequently become a first-line therapy for influenza, both for treatment and prevention, as well as becoming a multi-billion dollar prescription drug. Dr Kim is currently the Vice-President of Chemistry for Gilead Sciences. His current projects include antivirals, antibacterials, and immunosuppressants. He resides in the San Francisco area with his wife. His interests include hiking and travel.
Dr. Dennis C. Liotta is the Samuel Candler Dobbs Professor of Chemistry at Emory University. Prof. Liotta received his Ph.D. in Organic Chemistry in 1974 from The City University of New York under Dr. Robert Engel and completed his post-doctoral training at The Ohio State University under Dr. Leo A. Paquette. Dr. Liotta has been a professor at Emory University for thirty-four years. He is a Fellow of the Alfred P. Sloan Foundation, the recipient of a Camille and Henry Dreyfus Teacher Scholar Fellowship, an Alexander von Humboldt Senior Scientist Award, the 2005 Herty Award, and was the Emory University Distinguished Faculty Lecturer for 2006. Along with his colleague, Raymond Schinazi, he was the recipient of the 2003 Biomedical Industry Growth Award, given by the Georgia Biomedical Partnership. He is currently the Director of the Emory Institute for Drug Discovery, as well as the co-director of the Republic of South Africa Drug Discovery Training Program.
While at Emory, Dr. Liotta has authored over two hundred research publications and approximately seventy issued US patents. Over the last twenty five years he has also developed a great deal of experience in the discovery and development of pharmaceuticals. He has served as a consultant to several major pharmaceutical firms, including Merck, Glaxo, Burroughs Wellcome, Boehringer Ingelheim and Johnson & Johnson. He serves (or has served) on the Scientific Advisory Boards (SABs) of several small biopharmaceutical companies including Altiris (scientific founder), Pharmasset (scientific founder), iThemba Pharmaceuticals (scientific founder, SAB Chair), NeurOp, and FOB Synthesis. In addition, he is the inventor of record for several clinically important agents, including FTC (Emtriva®, Emtricitabine), 3TC (Epivir®, Lamivudine), Reverset® (DPC 817, D-D4FC), Racivir, Elvucitabine and MSX-122.
Dr. Victor E. Marquez was born in Caracas, Venezuela. He obtained a B.S. degree in Pharmacy in 1966 from Universidad Central de Venezuela and Master and Ph.D. degrees in Medicinal Chemistry from the University of Michigan in 1988 and 1970, respectively, under the tutelage of Professor Joseph H. Burckhalter. His career at the National Cancer Institute (NCI) started in 1971 when he joined as Visiting Fellow in the Medicinal Chemistry Section of the Developmental Therapeutics Program. During his NIH fellowship (1971-1972), while working under the supervision of Dr. John S. Driscoll, Dr. Marquez developed a novel hydantoin template for the delivery of nitrogen mustards specifically to the CNS. This research led to the design of the active brain antitumor agent, spiromustine. Phase I evaluation of spiromustine commenced in 1987, but neurotoxicity presented as alterations in cortical integrative functions led to its eventual withdrawal from further clinical use. Dr. Marquez then returned to Venezuela for a five-year period (1972-1976) where he worked as Director of Research in Laboratorios Cosmos, S.A. in Caracas. There, he developed a new class of orally active anaphylactic inhibitor, which was patented under U.S. pat. No. 4,167,577 in 1979. In 1977, Dr. Marquez rejoined the NCI as a Visiting Scientist and was awarded tenure as a Principal Investigator in 1987 after becoming a naturalized citizen. In 1988 he became Deputy Laboratory Chief and in 2000 he was promoted to Laboratory Chief. Dr. Marquez retired as Lab Chief on September 1, 2009 and is now Scientist Emeritus at the NCI. During his career at the NCI his discoveries have helped translate elements of basic research into solutions for specific medical problems as exemplified by cyclopentenyl cytosine (CPE-C) and 9-(2’,3’-dideoxy-2’-fluoro-beta-D-threo-pentofuranosyl)adenine, the latter also known as lodenosine. These drugs entered clinical trials in the late 1990’s and early 2000 as antitumor and anti-HIV drugs, respectively. They were later suspended from further clinical use due to unexpected toxicity. Currently, North-methanocarba thymidine, a potent antiherpes drug is schedule to enter phase I clinical trials. In addition, zebularine, a DNA methylase inhibitor, and 3-deazaneplanocin A, a histone methylase inhibitor, are important candidates under study for the epigenetic treatment of cancer. Other important discoveries that have resulted from his work in the area of nucleosides and nucleotides have been based on mechanistic approaches to inhibit key enzymatic reactions. Some of the most important highlights in this area are: (1) Design and synthesis of the most potent transition-state analogue inhibitors of cytidine deaminase based on a novel 5-hydroxy-perhydro-1,3-diazepin-2-one nucleoside system; (2) synthesis of thiazole-4-carboxamide adenine dinucleotide (TAD) and the corresponding metabolically stable phosphonate analogue (beta-methylene TAD), two of the most potent inhibitors of inosine monophosphate dehydrogenase; (3) synthesis and discovery of 3-deazaneplanocin A, the most potent inhibitor known against S-adenosylhomocysteine hydrolase; (4) synthesis and discovery of cyclopentenyl cytosine (CPE-C), the most potent inhibitor known to date against cytidine triphosphate synthase; (5) design and synthesis of the first, acid-stable dideoxypurine inhibitor of HIV reverse transcriptase; (6) design and synthesis of conformationally locked carbocyclic nucleosides as important biological probes; (7) design and synthesis of zebularine, an orally active DNA methylase inhibitor; and (8) design and synthesis of oligodeoxynucleotides containing conformationally restricted abasic sites as potent inhibitors of cytosine DNA methyltransferase. Concomitant to the work performed above, theoretical studies with conformationally locked nucleosides and oligonucleotides containing locked units have helped understand the role of sugar conformation in determining the affinity of nucleosides and nucleotides for kinases and polymerases. These studies have also set the basis for the design of delayed polymerase chain terminators effective against the scission repair mechanisms of resistant HIV reverse transcriptase. In a second line of research, Dr. Marquez developed a series of diacylglycerol mimetics, dubbed DAG-lactones that bind to the regulatory domain of protein kinase C (PKC) at nanomolar concentrations. Some DAG-lactones display isozyme selectivity for specific members of the PKC family and have shown potent antitumor activity in the NCI 60 cell line screen as well as exceptional apoptosis inducing properties. Dr. Marquez has received many awards and distinctions during his career, including the U.S. Department of Commerce Inventor’s award (1979); Medical Research Council Visiting Professorship at the Universities of Saskatchewan and Manitoba, Canada (1984-85); NIH Merit Award (1992); Vice-chair and Chair of Gordon Research Conference on Purines, Pyrimidines and Related Compounds (1993 and 1995); National Cancer Institute, Division of Basic Sciences Intramural Research Award (1997); Pharmazie-Wissenschaftpreiss 2001 (Pharmazeutische Chemie) sponsored by Phoenix Pharmahandel AG & Co (2001); Senior Biological Research Scientist appointment (2002); Member of the Medicinal Chemistry Division Long Range Planning Committee (2003-2005); Belleau Memorial Lecturer, McGill Chemical Society, McGill University (2003); Intramural AIDS Targeted Antiviral Program (IATAP) award (2005 and 2006); Leopoldo García-Colín-Scherer Medal, Mexico City, Mexico (2007); Symposium Honoring Victor Marquez for His Contributions to Conformational Analysis, Nucleosides, Nucleotides and Oligonucleotides, Division of Carbohydrate Chemistry, American Chemical Society, 236th National Meeting, Philadelphia, PA (2008); Elected Vice-President of the International Society for Nucleosides, Nucleotides and Nucleic Acids (2008); Maryland Chemist of the Year (2008); and Raymond U. Lemieux Lecture On Biotechnology, University of Alberta (2009). To date, the entire portfolio of his research is contained in more than 340 publications (71 in the Journal of Medicinal Chemistry with over 2476 citations), 11 book chapters, and 30 patents. Dr. Marquez has received over 120 invitations as a speaker to various symposia, universities and pharmaceutical companies.
Dr. Kenneth A. Jacobson received his B.A. in Liberal Arts from Reed College in Portland, Oregon and his M.S. and Ph.D. (1981) in Chemistry with Prof. Murray Goodman at the University of California, San Diego. After completing his Postdoctoral work with Professor A. Patchornik at the Dept. of Organic Chemistry, Weizmann Institute in Israel, he joined the National Institute of Diabetes & Digestive and Kidney Diseases at NIH in Bethesda, MD in 1983. He currently serves as Chief of both the Molecular Recognition Section, which he founded in 1993, and the Laboratory of Bioorganic Chemistry. He began the NIDDK Chemical Biology Core Laboratory as Director in 2003.
His creativity and his ability to combine the field of chemistry with those of pharmacology and molecular biology have had a major impact on biomedical research and therapeutic development. Over the course of two decades at NIH, Dr. Jacobson has made major contributions to the pharmacology of cell surface receptors, in particular purinergic receptors. He has studied recognition at the binding sites of G protein-coupled receptors (GPCRs) by structural modification, both from the perspective of the small molecular ligands and of their protein targets. His group began the computer modeling of adenosine receptors as a tool for interpreting site-directed mutagenesis data soon after their cloning. Early in his career he pioneered the concept of “functionalized congeners,” a now widely used approach in drug development, which has recently led to the design of multivalent conjugates of GPCR ligands using dendrimers as nanocarriers. He also introduced the concept of “neoceptors” as a strategy for re-engineering the binding site of a GPCR for activation by chemically tailored small molecules. His research has led to agents in clinical trials for cystic fibrosis, cancer, degenerative diseases, and autoimmune inflammatory diseases. Two nucleosides from the Jacobson laboratory that act as selective A3 adenosine receptor agonists are currently in clinical trials for rheumatoid arthritis, hepatocarcinoma, psoriasis, and dry eye disease. Dozens of ligands used as pharmacological probes in research on adenosine receptors and P2 (nucleotide) receptors were introduced by Dr. Jacobson and colleagues. Many of these substances bear the designation “MRS” after the name of his Section.
Dr. Jacobson has authored or co-authored over 500 scientific publications and is an inventor on 35 issued U.S. patents. He has served the ACS Division of Medicinal Chemistry as Chair in 2004 and has planned and chaired numerous symposia at ACS National Meetings. Dr. Jacobson is or has been on the editorial advisory boards of the Journal of Medicinal Chemistry, Bioconjugate Chemistry, Molecular Pharmacology, Current Topics in Medicinal Chemistry, Medicinal Research Reviews, and Future Medicinal Chemistry, and he is an Associate Editor ofPurinergic Signalling. He has mentored 63 postdoctoral fellows, both chemists and biologists. He received the 2003 Hillebrand Prize, the 2008 Sato International Memorial Prize from the Pharmaceutical Soc. of Japan, and the 2009 Pharmacia-ASPET Award from the American Soc. for Pharmacology and Experimental Therapeutics. Dr. Jacobson was recently included in a listing of the ten most cited researchers in the field of pharmacology.
Vice President of Basic Chemistry and Drug Discovery Sciences, and the Deputy Site-Head of the Rahway Site
Dr. Malcolm MacCoss obtained his Ph.D. in organic chemistry from the University of Birmingham in the U.K. in 1971, working with Professors A.S. Jones and R.T. Walker and then carried out a post-doctoral fellowship and a research associateship at the University of Alberta in Canada from 1972-1976 working with Professor M.J. Robins. During those times he worked in the field of nucleoside and nucleic acid chemistry, including synthetic and hybridization studies on oligonucleotides that contained a non-ionic backbone, as well as developing novel synthetic methods in nucleoside chemistry. He then moved to the U.S.A. and took up an appointment at Argonne National Laboratory in Illinois where he continued to work on nucleic acid chemistry and the solution structures of nucleic acid components by NMR spectroscopy. In particular, he studied the synthesis and solution conformation of a number of rigid nucleoside cyclic monophosphates. In 1980, also while at Argonne, he won the University of Chicago Medal for Distinguished Performance at Argonne National Laboratory (awarded to scientists under 40 years old) for his work on novel phospholipid-nucleoside conjugates as prodrugs for anticancer agents. During this time he also held an Adjunct Associate Professorship in Medicinal Chemistry at the University of Illinois Medical Center, Chicago.
Dr. MacCoss began his pharma career at Merck as a Research Fellow in 1982 and he was promoted to Assistant Director, Exploratory Chemistry in 1986; to Director, Medicinal Chemical Research in 1991; to Senior Director and Head of Medicinal Chemical Research in 1993; to Executive Director, Medicinal Chemistry in 1995; and to Vice President Basic Chemistry-Rahway in 1999. In 2003, he became the Vice President of Basic Chemistry and Drug Discovery Sciences, and the Deputy Site-Head of the Rahway Site; he was also Chairman of the Merck World-Wide Chemistry Council. During his time as Head of the Merck Rahway Chemistry Department, the Department produced approximately 100 preclinical drug candidates. In March, 2008 Dr. MacCoss retired from Merck and spent a short time as a private consultant. In July, 2008 he was appointed Group Vice President for Chemical Research at the Schering-Plough Research Institute. In this role, he provides strategic leadership to the Chemistry Research group globally and is the Head of Chemistry at the Schering-Plough, Kenilworth, NJ site. In addition, he chairs the newly created Schering-Plough Global Chemistry Council, a forum for formulating global chemistry strategies. Dr. MacCoss also serves on the Advisory Council for the Executive Dean of the School of Arts and Sciences at Rutgers University, and on the Advisory Board of the Rutgers University Chemistry and Chemical Biology Department.
When he was an active project leader at Merck, Dr. MacCoss led a medicinal chemistry group that synthesized the first oral Substance P antagonist, Emend™ (aprepitant), which is a Merck anti-emetic product approved by the FDA in 2003 for the treatment of chemotherapy induced nausea and vomiting, for which he was awarded the Thomas Edison Award in 2004, along with the other inventors. In addition, his group prepared the novel IV prodrug of Emend (Ivemend™, fosaprepitant), which was approved by the FDA in January 2008. In 2007, Dr. MacCoss was awarded a second Thomas Edison Award, for his contributions to the inventorship of Januvia™ (sitagliptin phosphate), the first approved DPP-IV inhibitor for the treatment of type 2 diabetes. Januvia™ was approved in 2006 and a fixed dose combination of Januvia™ and metformin (Janumet™) was approved in 2007. Most recently, in March 2008, Dr. MacCoss was awarded the NJ American Chemical Society Award for Creativity in Molecular Design and Synthesis; he was admitted as a Fellow of the Royal Society of Chemistry (FRSC) in 2008.
Dr. MacCoss has authored or co-authored 152 publications in refereed journals, he is an inventor on 93 issued U.S. patents, has authored 8 book chapters and has been an invited speaker 44 times at major symposia or at universities and industrial venues. He and his wife Sandy have 2 children, both of whom are professional scientists (Dr. Michael MacCoss is a protein mass spectroscopist and an Associate Professor of Human Genome Sciences at the University of Washington, Seattle, WA, and Dr. Rachel MacCoss is a synthetic chemist in the pharmaceutical industry in Boston, MA).
Richard B. Silverman is the John Evans Professor of Chemistry at Northwestern University. Professor Silverman received his B.S. degree in chemistry from The Pennsylvania State University in 1968 and his Ph.D. degree in organic chemistry from Harvard University (David H. Dolphin, mentor) in 1974 with time off for a two-year military obligation from 1969-1971. After two years as a NIH postdoctoral fellow in the laboratory of the late Professor Robert H. Abeles in the Graduate Department of Biochemistry at Brandeis University, he joined the chemistry faculty at Northwestern University. In 1986 he became Professor of Chemistry and Professor of Biochemistry, Molecular Biology, and Cell Biology. In 1996 he was named the Arthur Andersen Professor of Chemistry for a period of two years and since 2004 he has been the John Evans Professor of Chemistry. He has supervised 125 graduate students and postdoctoral associates at Northwestern.
Professor Silverman’s research can be summarized as investigations of enzyme mechanisms and the molecular mechanisms of action, rational design, and syntheses of potential medicinal agents, particularly for central nervous system diseases. Dr. Silverman has formulated and tested new enzymatic hypotheses with the use of novel organic chemical approaches to elucidate enzyme-catalyzed reactions, to design mechanism-based inactivators of enzymes, and to understand the molecular mechanisms of inactivation of enzymes. The enzymes that he studies are not only mechanistically interesting, but also highly relevant to pharmaceutical inhibitor design. For example, with the use of a variety of novel mechanism-based inactivators, Dr. Silverman pioneered and developed the mechanistic work that led to a radical mechanism for the enzyme monoamine oxidase. When he first reported his results in 1980, radical involvement in enzyme-catalyzed reactions was rarely proposed and poorly understood. It is now apparent that radical intermediates in enzyme-catalyzed reactions are quite prevalent.
Detailed mechanisms of inactivation of γ-aminobutyric acid (GABA) aminotransferase, the enzyme that degrades the inhibitory neurotransmitter GABA, were elucidated by Dr. Silverman. Compounds that inhibit this enzyme raise the brain levels of GABA, which has an anticonvulsant effect. Over the years he has demonstrated that few inactivators proceed by a single inactivation mechanism. For example, he showed that the antiepilepsy drug, vigabatrin (Sabril™), inactivates GABA aminotransferase by three different pathways.
For a compound to act as a drug that inhibits GABA aminotransferase, it is imperative that it does not also inhibit the enzyme responsible for the production of GABA, namely glutamate decarboxylase; otherwise, this would defeat the purpose of inhibiting its degradation. The other important feature of a potential CNS drug is its ability to enter the brain. A series of compounds was designed by Professor Silverman to inhibit GABA aminotransferase without inhibition of glutamate decarboxylase and to have increased lipophilicity for brain penetration. Unexpectedly, these compounds activated glutamate decarboxylase and produced additional GABA. These compounds were tested for anticonvulsant activity because of this potential new mechanism to increase brain GABA levels, and one of them, after an additional 14 years of testing in animals and in humans, became Lyrica™ (pregabalin), the first FDA-approved treatment for diabetic neuropathy, postherpetic neuralgia, and fibromyalgia; it is also effective in the treatment of epilepsy.
Other early enzyme studies in Professor Silverman’s lab include model studies for the mechanism of vitamin K epoxide reductase and orotidine 5’-phosphate decarboxylase and investigations of the mechanism and inactivation of nitric oxide synthase (NOS), an enzyme important for regulation of the blood pressure, the immune defense system, and brain development and memory. Excess production of nitric oxide, however, is implicated in numerous neurodegenerative diseases. Professor Silverman designed the first dual-selective inhibitors of the neuronal isozyme of NOS and used these in collaboration with the crystallography group of Thomas Poulos at the University of California, Irvine to obtain crystal structures of these potent and selective reversible inhibitors. The obtained structures were employed to develop a new fragment-based de novo design of a class of more potent and selective compounds that have been found to be remarkably active in a rabbit model for cerebral palsy.
Professor Silverman has received numerous awards for research: DuPont Young Faculty Fellow (1976), Alfred P. Sloan Research Fellow (1981-1985), NIH Research Career Development Awardee (1982-1987), Fellow of the American Institute of Chemists (1985), Fellow of the American Association for the Advancement of Science (1990), Arthur C. Cope Senior Scholar Award of the American Chemical Society (2003), Alumni Fellow Award from The Pennsylvania State University (2008), and the Perkin Medal from the Society of Chemical Industry (2009). He also is the recipient of several teaching awards including the E. LeRoy Hall Award for Teaching Excellence (1999), the Excellence in Chemistry Education Award from the Northwestern University Chapter of Alpha Chi Sigma Chemistry Fraternity (1999), the Northwestern University Alumni Teaching Award (2000), and the Charles Deering McCormick Chair in Teaching Excellence (2001). Professor Silverman also was awarded a U.S. Army Commendation Medal for meritorious service (1971).
Editorial Advisory Boards on which Professor Silverman has served include the following journals: Current Enzyme Inhibition (2004-present), Bioorganic & Medicinal Chemistry (2003-present), Bioorganic & Medicinal Chemistry Letters (2003-present), Letters in Drug Design & Discovery (2003-present), Archiv der Pharmazie- Pharmaceutical and Medicinal Chemistry (1995-present), Journal of Enzyme Inhibition and Medicinal Chemistry (1988-present), Archives of Biochemistry and Biophysics (1993-2003), and Journal of Medicinal Chemistry (1995-2000).
Dr. Silverman has published over 250 research articles and reviews, holds 41 domestic and foreign patents, and has written four books (one translated into German). His book entitled “The Organic Chemistry of Drug Design and Drug Action” is in its second edition. From 1992-2006 he gave two-day short courses on drug design and drug action at the national meetings of the American Chemical Society, as well as at various pharmaceutical companies. He has been a lecturer at the Residential School on Medicinal Chemistry (Drew University) since 1995, presenting lectures on enzyme inhibition and on lead modification. He was elected nominating committee (1990), treasurer (1993-1996), and program chair (2001) of the Division of Biological Chemistry of the American Chemical Society and canvassing committee (1982-1987; chair 1987) and long-range planning committee, Division of Medicinal Chemistry of the American Chemical Society.
Professor of Medicinal Chemistry & Director of Temple University’s Center for Drug Discovery Research
Magid Abou-Gharbia is currently Professor of Medicinal Chemistry and Director of Temple University’s Center for Drug Discovery Research. He recently retired from Wyeth Research as senior vice president of Chemical and Screening Sciences, following a very successful 26-year career, where he built a strong multi-disciplinary organization. During his tenure he fostered a highly creative environment based on modern drug discovery technologies and enhanced chemistry skills and capabilities via the recruitment of high caliber scientists. Under his leadership, his group research efforts led to the discovery of six marketed drugs and many compounds currently under clinical evaluation including: first-in-class antidepressant Effexor®; Anticancer Agent Mylotarg®, a sedative hypnotic Sonata®; a broad spectrum antibiotic Tygacil®, an anticancer rapamycin derivative, Torisel™ and an SNRI antidepressant, Pristiq®. His scientific accomplishments include over 175 invited lectures, presentations and publications. He is an inventor on 99 issued US patents and over 350 patents worldwide. As a result of this Magid was named in list of most prolific inventors by US Patent & Trademark association. He received a number of awards, including the Alfred Burger Award in Medicinal Chemistry (2008), American Institute of Chemists (AIC) Chemistry Pioneer Award (2007), Researcher of the Year (2006) from Health Care Institute of NJ (HINJ); Trailblazer Award (2006) from Science Spectrum; Induction into the New Jersey Inventors Hall of Fame (2004); the Procter Medal (2003); ACS Earle B. Barnes Award (2001); Philadelphia Organic Chemists Club (POCC) Award (2001); Egyptian Pharmaceutical Society Drug Discovery Award (2000). As a mentor, Magid developed leaders at all levels throughout Chemical and Screening Sciences. He actively encouraged his colleagues at Wyeth to contribute to and participate in American Chemical Society activities, and was a strong supporter of the Division of Medicinal Chemistry in the form of session, meeting and graduate fellowship sponsorship.
Raymond E. Counsell was born in Vancouver, British Columbia, Canada. He received his Bachelor of Science in Pharmacy degree from the University of British Columbia in 1953 and his PhD in Medicinal Chemistry and Organic Chemistry from the University of Minnesota in 1957. From 1957 to 1964 he served as Senior Research Chemist at G. D. Searle and Company in Skokie, IL.
Searle’s research was heavily involved in steroid chemistry. Ray was placed in Frank Colton’s group which was active in the development of contraceptive agents and anabolic steroids. Ray was encouraged to develop his own research program. His early efforts involved pursuing structure-activity relationships among the 19-norsteroids which have the basic structure known as estrane. This led to one of his earliest papers entitled “Isomeric Estrane Derivatives” published in Tetrahedron in 1961. This paper was notable for providing the first chemical and biological properties for substituted 5α, 10α-estranes. Other studies on anabolic steroids were conducted in collaboration with colleague Dr. Paul Klimstra and summarized in their chapter in Alfred Burger’s third edition of Medicinal Chemistry (1970).
His next major effort involved a search for agents to regulate cholesterol biosynthesis for the treatment of atherosclerosis. Based on publications which indicated that feeding cholesterol to animals limited the rate at which the sterol was synthesized in the liver led Counsell to design and synthesize agents that would mimic cholesterol in this feedback process. This encouraged him to prepare a series of azacholesterols. One of these was 20,25-diazacholesterol which appeared promising in animal studies, but had a brief exposure in the clinic because of side effects (muscle cramping). Subsequent studies by Counsell and his students revealed 20,25-diazacholesterol to be a potent inhibitor of cholesterol side-chain cleavage, a key step in the biosynthesis of the female and male sex hormones (J. Med. Chem., 1972). In recent years 20,25-diazacholesterol under the name of Ornitrol or Diazacon has been used as a contraceptive to control pigeon populations as well as those of other annoying small animals under the auspices of the USDA National Wildlife Research Center.
In 1963, Counsell was asked to consider joining the Nuclear Medicine group at the University of Michigan Medical School to establish a new program in the design and synthesis of radiopharmaceuticals for tumor and organ imaging (currently known as Molecular Imaging). An award from the American Cancer Society provided support for his appointment as Associate Professor of Medicinal Chemistry in the College of Pharmacy and Department of Internal Medicine in the Medical School with full tenure. Research funding from N.I.H. provided the resources to establish his research program. His groups efforts led to radioiodinated 19-iodocholesterol which became the first agent to noninvasively visualize the adrenal gland and associated tumors in humans ( J. Nucl. Med., 1970). Prior to that, a radioiodinated analog of chloroquin gave rise to the first agent to produce clinical images of malignant melanoma in patients (J.A.M.A., 1968). This agent was licensed to Mallinckrodt Pharmaceutical where it was marketed under the name of Iomethin-131 and used for many years by the National Eye Institute for the diagnosis of uveal melanoma.
Counsell’s continued interest in synthesizing agents to regulate steroid hormone biosynthesis led his laboratory to prepare and evaluate inhibitors of the enzyme aromatase, a key enzyme in the biosynthesis of the estrogen hormones. This led to a number of potent inhibitors which were among the few known at the time (J. Med. Chem., 1978). These studies were conducted by Robert Brueggemeier for his doctorate and have been expanded by him in his laboratory at Ohio State University.
Further studies with radioiodinated derivatives of cholesterol led to the recognition of the importance of plasma lipoproteins in their biodistribution and tissue uptake by receptor-mediated endocytosis. This led to the concept that certain types of lipoproteins could be useful carriers for radiodiagnostics (see perspective article in J. Med. Chem., 1982). This concept was perfected by colleagues Weichert and Longino in the Department of Radiology. This technology was subsequently licensed by the University of Michigan and has given rise to two products known as Fenestra LC for liver imaging and to a pegylated version known as Fenestra VC for vascular contrast enhancement. (For animal use only at this time).
Counsell’s most recent efforts have involved radioiodinated phospholipid analogs for tumor imaging. Early publications (J. Med. Chem., 1989) demonstrated the remarkable ability of these agents to selectively concentrate in tumors. Several more years of chemistry, animal studies and tests in patients finally gave rise to the most tumor selective agent known as NM-404 (J. Med. Chem., 2006). The University of Michigan has licensed a company known as Cellectar to commercialize NM-404 for the diagnosis and treatment of cancer.
Dr. Counsell’s studies have been reported in over 250 peer-reviewed publications and 21 book chapters, and he holds over 50 U. S. Patents. During the course of his investigations, 25 graduate students have received Ph.D. degrees from the University of Michigan along with 12 others who received their Masters degree with Dr. Counsell serving as their thesis chair. Thirty-five postdoctoral fellows have also trained with Dr. Counsell.
Dr. Counsell has served on the editorial boards of the Journal of Medicinal Chemistry, Journal of Pharmaceutical Sciences and the Quarterly Journal of Nuclear Medicine. In addition he has served as a senior editor for the Journal of Medicinal Chemistry and as a section editor for the Annual Reports in Medicinal Chemistry. He has been active in the American Chemical Society Division of Medicinal Chemistry and served as chair from 1970-71, the Academy of Pharmaceutical Sciences where he served as Chair of the Section of Medicinal Chemistry from 1970-71, the Society of Nuclear Medicine, and the International Association of Radiopharmacology where he served as president from 1994-95.
In the Department of Pharmacology, Dr. Counsell served as acting chair from 1987-88, as associate chair from 1988-90, and as interim chair from 1990-94. He has also been active in the Interdepartmental Program in Medicinal Chemistry and one in which he assisted Professor Burckhalter organize in the 1960s. This graduate program received an N.I.H. Training grant in 1968 which has continued to this day. He served as interim chair of the interdepartmental program from 1973-76.
Among his honors and awards are listed the Horner Gold Medal in Pharmacy (1953), the American Cancer Society Research Associate Award (1964-71), American Cancer Society Eleanor Roosevelt International Fellowship (1972), the Czerniak Prize of Nuclear Medicine and Radiopharmacology, the Fogarty International Fellowship (1986), the T. O. Soine Memoral Award (1981) and Alumni Outstanding Achievement Award (1989) from the University of Minnesota. He has been elected as a fellow in the Academy of Pharmaceutical Sciences (1973), AAAS (1980), and the American Association of Pharmaceutical Sciences (1987). In 2003 he was awarded the Technology Transfer Career Achievement Award from the University of Michigan.
During his academic career he served on numerous university and National committees. From 1968 to 1972 he was a member of the NIH Medicinal Chemistry Study Section A and from 1975 to 1979 he was a member of the Pharmacology-Toxicology Program Committee of NIGMS. From 1979 to 1983 he was a member of the Committee on Medical Radioisotopes for Los Alamos Scientific Laboratories.
On September 1996 the Regents of the University of Michigan named Dr. Counsell Professor Emeritus of Pharmacology and Medicinal Chemistry.
Distinguished Research Fellow & Team Leader in Johnson & Johnson Pharmaceutical Research & Development, Spring House, Pennsylvania
Dr. Bruce E. Maryanoff was born on 26 February 1947 in Philadelphia, Pennsylvania. While growing up in Philadelphia, he established his first “laboratory” in the basement of his home at eight years of age. These early chemical studies eventually brought some dismay to his parents, due to nasty odors and shock-sensitive compounds. From Drexel University, Dr. Maryanoff earned a B.S. degree in chemistry (1969) and a Ph.D. degree in organic chemistry (1972; with Prof. Robert O. Hutchins). In 1971, he married Dr. Cynthia A. Maryanoff (née Milewski), an organic chemistry labmate. After postdoctoral studies for two years at Princeton University with Prof. Kurt M. Mislow, he joined McNeil Laboratories, Inc., a Johnson & Johnson subsidiary. He advanced on the scientific ladder in various Johnson & Johnson pharmaceutical units to the highest scientific position in the company. Presently, he is a Distinguished Research Fellow and a Team Leader in Johnson & Johnson Pharmaceutical Research & Development, Spring House, Pennsylvania.
Dr. Maryanoff has made numerous contributions in medicinal chemistry and organic chemistry. He is an internationally renowned expert in drug design and drug discovery. From 1976−1992, he focused on central nervous system (CNS) therapeutics, with an emphasis on anticonvulsants and antidepressants. Dr. Maryanoff invented TOPAMAX® topiramate, a unique sugar sulfamate derivative, which is marketed worldwide for treating epilepsy and migraine headache, and achieved annual sales of more than $2 billion. Since 1991, he has pursued cardiovascular therapeutics, while also seeking drugs for treating pulmonary inflammatory diseases, metabolic disorders, and epilepsy. In the past 15 years, his drug research has dealt with structure-based drug design; peptides and peptidomimetics; inhibitors of diverse enzymes, especially serine proteases (thrombin, factor Xa, tryptase, cathepsin G, chymase) and kinases (protein kinase C-β, glycogen synthase kinase-3β); integrin (GPIIb/IIIa, αvβ3/5, α4β1/7) antagonists; and ligands for G-protein-coupled receptors (protease-activated receptors, urotensin-II receptor, vasopressin receptors, ADP receptor P2Y12). His efforts have led to 23 compounds entering preclinical development, 13 of which advanced into human clinical trials. In organic chemistry, he made seminal contributions to understanding the stereochemistry and mechanism of the Wittig olefination reaction; adapted cobalt-mediated [2+2+2] alkyne cyclotrimerizations to the synthesis of macrocycles; and devised novel, self-assembling collagen-mimetic peptides. Dr. Maryanoff has published 260 scientific papers, is an inventor on 95 U.S. Patents (issued or pending), has presented 160 invited lectures, and has mentored 11 postdoctoral associates.
Dr. Maryanoff has served in numerous capacities, including: the Editorial Advisory Boards of 12 journals; a 4-year term on the Medicinal Chemistry Study Section of the National Institutes of Health; a 4-year term on the Advisory Board of the American Chemical Society (ACS) Petroleum Research Fund; Chairman of the 1989 Gordon Research Conference on Organic Reactions and Processes; member of the Board of Directors of the ACS Philadelphia Section; and Chair of the Philadelphia Organic Chemists’ Club. He has organized and chaired several symposia at ACS national and regional meetings, edited a special issue of J. Med. Chem. to honor the memory of Dr. Paul A. J. Janssen (published in 2005), and was the inaugural editor of the book series Advances in Medicinal Chemistry.
Awards & Honors
Dr. Maryanoff has received two ACS national awards, a 2000 ACS Heroes of Chemistry Award and the 2003 ACS Award in Industrial Chemistry. He was inducted into the ACS Medicinal Chemistry Division Hall of Fame in 2008. He received a Philadelphia ACS Section Award (1984) and a Philadelphia Organic Chemists' Club Award (1995). He was honored with the Johnson Medal for Research and Development for discovery and development of TOPAMAX®, and was twice a recipient of Johnson & Johnson's Philip B. Hofmann Research Scientist Award. Dr. Maryanoff was recognized by Drexel University as a notable alumnus with several awards, including election to the Drexel Alumni 100 Club. He was elected a Fellow of the American Association for the Advancement of Science (1989) and a Fellow of the Royal Society of Chemistry (2000).
Van Vleet Endowed Chair of The Department of Pharmaceutical Sciences & Associate Dean of Graduate Study and Research in the College of Pharmacy at the University of Tennessee, Health Science Center, Memphis TN. Dr
Professor Duane D. Miller is currently the Van Vleet Endowed Chair of The Department of Pharmaceutical Sciences and Associate Dean of Graduate Study and Research in the College of Pharmacy at the University of Tennessee, Health Science Center, Memphis TN. Dr. Miller obtained his B.S. degree at Kansas University in 1966, and his interest in research was stimulated as a National Science Foundation Undergraduate Research Fellow. He was an NIH Fellow while at the University of Washington working under the direction of Dr. Wendel L. Nelson and obtained his Ph.D. in 1969. He joined The Ohio State University Faculty in 1969, where he became Chairman of the Division of Medicinal Chemistry and Pharmacognosy in 1982. He moved to the University of Tennessee, Health Science Center, Memphis, TN in 1992. Dr. Miller has published over 250 publications with graduate students, research associates, and scientific collaborators. He has 14 book chapters and has given 320 presentations at national and international meetings and has 30 US patents. He has trained 30 Ph.D. and Master Degree students and has worked with over 30 postdoctorals and research assistants.
Dr. Miller’s research interests include the design and synthesis of new drug molecules. He has a strong interest in stereochemical aspects of drug molecules and developing drugs for new areas in which we currently lack therapeutic agents or in areas in which we need to develop new drugs with fewer side effects. Dr. Miller’s laboratory reported on the first nonsteroidal androgen agonists in collaboration with Dr. Jim Dalton, formerly with The Ohio State University and currently employed at GTx, a Biotech Company in Memphis. They discovered the new nonsteroidal selective androgen receptor modulators (SARMs) and reported on them in 1998. This work came about through the use of NIH and Van Vleet Endowed Chair funds on understanding how androgen antagonists bind to the androgen receptor. They made an observation that some of the new nonsteroidal agents that they had synthesized were not blocking but were actually stimulating androgen receptors. They have 10 issued patents and other technical material that has been licensed to GTx by the University of Tennessee. They are now working with GTx, an exciting new company in Memphis, under the direction of Dr. Mitch Steiner to get therapeutic agents on the market in the SARM area. The SARMs are now in Phase II human clinical testing. Recently, Merck has partnered with GTx in trying to bring these new agents to market. These agents can be used for muscle wasting and osteoporosis. The new SARMS have the advantage that they are orally active with fewer side effects, including less liver toxicity than current muscle building agents. Such agents may be of value in aging males to treat low testosterone in older males, [called ADAM (androgen decline in aging males) or also called andropause].
Dr. Miller is currently working with Dr. Gabor Tigyi, in the Department of Physiology, on NIH funded ligands for lysophosphatidic acid (LPA) and demonstrating how this new class of agents can be used therapeutically. The work with LPA anlaogs, at the University of Tennessee, has led them to set up a company called RxBio that is focused on licensing and developing new drugs to interfere or prevent the side effects of chemotherapy and radiation therapy on the GI tract. The company was founded by Dr. Gabor Tigyi, Dr. Rusty Johnson, Dr. Shannon McCool and Dr. Miller in 2000.
In 2002 Dr. Miller confounded ED laboratory Inc. along with Dr. Eldon Geisert and Dr. Shannon McCool. This company is focused on anticancer agents discovered by Dr. Miller and Dr. Geisert at the University of Tennessee and licensed to ED laboratory. These new agents are of great interest in treating brain cancer (gliomas). Dr. Ryan Yates, also in the Department of Pharmaceutical Sciences at the UT has been very instrumental in aiding in the design of a second generation of brain cancer agents for the company. Dr. Miller has worked with Dr. Dennis Feller, originally at The Ohio State University and currently at the University of Mississippi, for over 30 years in discovering agents for obesity/diabetes and more recently with Dr. Bill Purcell in a company called Thinline, LLC, located in Memphis. In a very recent collaboration with Dr. Ryan Yates (2007), they discovered a new chemical class of anti-inflammatory agents that should have fewer side effects than the classical steroidal anti-inflammatory agents used today. In efforts to find new therapeutic agents for the treatment of melanoma, he is working with Dr. Wei Li in searching chemical libraries to find new anticancer agents and designing new molecules around those leads.
During his academic career Dr. Miller was presented the University of Tennessee National Alumni Outstanding Teacher Award (1994). He was made a Charter Member of the Academy of Distinguished Teaching and Service Professors at The University of Tennessee, Health Science Center (1999), and he has been honored by the Student Government Association Executive Council (SGAEC) Excellence in Teaching Awards In 1995 and 2006. He was presented the Otto and Kathleen Wheeley Award for Excellence in Technology Transfer in 2005. He was honored as an American Association Pharmaceutical Scientists (AAPS) Fellow in 1990. He was selected as an American Association for the Advancement of Science (AAAS) Fellow and honored for fundamental studies on the structural and stereo-chemical requirements of adrenergic drugs interacting in the CNS and peripheral nervous systems (2001).
Born in Munich, Germany, John Neumeyer immigrated to England in 1939 and to the USA in 1945. In New York City he graduated from The Bronx H.S. of Science (1948) and then received his B.Sc. from Columbia University (1952). He completed his studies in 1961 receiving his Ph.D. in Medicinal Chemistry from the University of Wisconsin.
As a research chemist at Ethicon Inc, he was awarded the basic patents for the aluminum foil suture package required for gamma radiation sterilization. Neumeyer was hired by FMC Corporation in 1961 to work on synthetic pyrethroids and their synergists and, in 1963, moved to Cambridge, MA to work at the consulting firm of Arthur D. Little, Inc. In 1969, he received a joint appointment at Northeastern University as Professor of Medicinal Chemistry and Chemistry.
Professor Neumeyer’s research first attracted attention because of his studies of the chemistry of aporphines which resulted in the first total syntheses of racemic apomorphine, apocodeine and N-n-propylnorapomorphine (NPA). He developed the first electrochemical and photochemical cyclization routes to aporphines. Neumeyer then focused his attention on the development of ligands for the in vivo visualization of the dopamine transporter and/or the cocaine receptor site. The first report of a high affinity radioactive ligand, [3H]-CFT, a phenyltropane derivative, was reported from his laboratory in 1989. Further development of this tritiated ligand led to a series of studies which culminated in the development of the [123I], [18F] and [11C] phenyltropanes, CIT and FP-CIT (DaTSCAN™, ioflupane). These commercially available ligands are used for the diagnosis of Parkinson’s disease.
An important aspect of Professor Neumeyer’s career was his role as cofounder and Scientific Director of Research Biochemicals International (RBI) in 1980. His objective in founding this company was to make non-radioactive ligands available to the scientific community. RBI gained worldwide respect and recognition as the leading source of neurochemicals. The RBI Handbook of Receptor Classification, co-edited by Neumeyer and Kebabian, is now in its fifth edition.
Professor Neumeyer has received numerous awards including: the Lunsford Richardson Prize for his Ph.D. thesis (1961); Pfeiffer Memorial Research Award (1975); Senior Hayes Fulbright Fellowship (1975); Northeastern University Faculty Lecturer (1978); first Matthews Distinguished University (Northeastern) Professor (1980); Academy of Pharmaceutical Sciences Research Achievement Award in Pharmaceutical and Medicinal Chemistry (1982); and the Marie Curie Award of the European Association of Nuclear Medicine (1992). He has served on the Committee of Revision of the U.S. Pharmacopoeia (1970-1985) and various NIH study sections.
Neumeyer founded the Medicinal Chemistry Group in the Northeastern Section, ACS, (1965); Chaired the Division of Medicinal Chemistry (1982); and Chaired the Northeastern Section of the ACS (2003). In 1998, Neumeyer received the Henry A. Hill Award for Outstanding Service to the Northeastern Section. He has served on the editorial advisory boards of several journals including The Journal of Medicinal Chemistry where he was the first book review editor.
During the course of his career Professor Neumeyer has trained approximately 60 graduate students and postdoctoral fellows. He is the author of more than 300 refereed scientific publications and 22 US patents. As Distinguished Emeritus Professor, he continues his research activities at Harvard Medical School in the Alcohol and Drug Abuse Research Center of McLean Hospital where he serves as Director of the Medicinal Chemistry Program.
Professor and Chair of the Department of Medicinal Chemistry to the University of Kansas
Edward E. Smissman was born on July 29, 1925, in East St. Louis, Illinois. Upon his graduation from East St. Louis High School in 1941, he enlisted in the U. S. Coast Guard. After 3½ years of service he began his academic training, earning his B.Sc. in 1948 from the University of Illinois, and his Ph.D. in organic chemistry from the University of Wisconsin in 1952 with Eugene van Tamelen.
In early 1952, Ed and his wife, Clare, moved from Madison, Wisconsin to Chicago, Illinois, where he assumed his first academic position as Assistant Professor at the University of Illinois College of Pharmacy. In 1955, Ed accepted a position at the University of Wisconsin, where he began to build a graduate program in medicinal chemistry. Ed’s wide range of scientific interests were evident in the variety of research activities he carried out. He not only continued his doctoral research on the isolation, structural studies, and synthesis of natural products, but also began working in the area of organic reaction mechanisms and aspects of stereochemistry. While at Wisconsin, he began his investigations of host-plant-resistance factors which led to the development of his program in insect chemistry. He also initiated his studies of the mechanism and stereochemistry of the Prins reaction and the quasi-Favorskii rearrangement. In addition to these long-range interests, a variety of other problems, including the stereospecific syntheses of shikimic and quinic acids, were studied. Such diversity of research activity created a stimulating and challenging atmosphere in Ed’s laboratories.
In 1960, Clare and Ed moved to The University of Kansas, where he became Professor and Chair of the Department of Medicinal Chemistry. He continued his work in natural products and synthetic chemistry, but he became intensely interested in conformational aspects of autonomic receptor sites, and a series of papers began to appear describing work in this area. In 1964, Ed was named a University Distinguished Professor.
Ed was an innovator of interdisciplinary research at KU. He had the unique ability to be able to bring together individuals in different disciplines and create an environment of cooperation and creativity. His success in this capacity was demonstrated by the Health Sciences Advancement Award, which the National Institutes of Health granted to KU in 1969. This grant, largely the result of Ed’s efforts, resulted in a significant increase in the number of faculty positions in the chemical & biological science at KU and in the construction of McCollum Laboratories, a building used as a center of interdisciplinary research at KU. At the time of his death, Ed was spearheading a second proposal that led to the establishment of the Center for Biomedical Research, the forerunner of the Higuchi Biosciences Center, and to the construction of the Smissman Research Laboratory building.
Ed’s energy was limitless, his enthusiasm boundless, and his devotion to his students, colleagues, and science was infinite. He was author or coauthor of over one hundred research publications covering a wide variety of topics in medicinal chemistry. He participated directly in the training of over seventy Ph.D. students, and twenty postdoctoral fellows, and influenced the lives of many others. It is impossible to overestimate the extent of this influence. He had colleagues and friends all over the world whose lives were enriched by knowing him.
Ed felt a strong responsibility to be active in his professional associations. He served first as vice-chair and chair of the long-range planning committee of the Division of Medicinal Chemistry of the American Chemical Society and became chair of the Division in 1959. He was General Chair of the Sixth National Medicinal Chemistry Symposium, Counselor in the Division of Medicinal Chemistry for many years, and served on the editorial boards of the Journal of Medicinal Chemistry, Annual Reports in Medicinal Chemistry, and the American Chemical Society Advances in Chemistry series. He also took an active role in the Medicinal Chemistry Section of the Academy of Pharmaceutical Sciences. In 1972–74, he served as chair of the IUPAC Committee on the International Education of Medicinal Chemists. Because of his extraordinary talents as a researcher and teacher, Ed was in demand as a lecturer throughout the world at conferences and universities and as a consultant at industrial laboratories. In addition, he spent many years as a member of National Institutes of Health study sections and panels.
Ed died unexpectedly on Sunday, July 14, 1974. He was not quite forty-nine years old. His qualities as a teacher, a scientist and a human being inspired generations of students and affected all who knew him. His influence will not soon be forgotten. The atmosphere of cooperation and goodwill which Ed fostered at KU will remain as his greatest memorial.
Clarine Feir was born in 1926 in St. Louis, Missouri. She earned a bachelor’s degree at The Ohio State University. She and Ed were married in 1951 while Ed was in graduate school. They were second parents to all the graduate students and postdoctoral fellows in the department. They entertained often in their home (shared with Hagen, their handsome German Shepherd), and Clare accompanied Ed on most of his travels. She obtained a law degree at KU in 1966 and practiced law in Lawrence and Baldwin City where she also was on the faculty at Baker University. After Ed’s death she earned an MBA degree at KU and moved to Winter Park, Florida where she remarried (William Robinson), practiced law and taught business law part-time at Rollins College. Following her death in 2004, the Smissman Memorial Fund was renamed as the Edward E. and Clarine F. Smissman Memorial Fund.
It was Clare’s wish that, as a lasting tribute to a great man, the Edward E. Smissman Lecture Series in Medicinal Chemistry be established. By sponsoring lecturers of outstanding merit and achievement in chemistry and biology, it is hoped that the influence and tradition of both Ed and Clare Smissman will be preserved.
Vice President, Chemistry, responsible for the scientific direction of the Merck Frosst Laboratories
Dr. Burton G. Christensen was born in Waterloo, Iowa (April 8, 1930) and received his B.Sc. degree in chemistry from Iowa State University (1952) followed by his A.M. and Ph.D. degrees (1956) in organic chemistry from Harvard University. He went directly to the Merck Research Laboratories of Merck & Co., Inc., where his final positions was Senior Vice President, Chemistry, directing ongoing basic research on human, animal health, and agricultural chemical projects, as well as being responsible for the scientific direction of the Merck Frosst Laboratories.
His early research was in the areas of diazoketone, steroid and heterocyclic chemistry. However, since about 1965 his interests have been concentrated in antibiotic chemistry. Before 1970 his most notable work was concerned with the structural elucidation, synthesis and analog syntheses of the antibiotic fosfomycin (phosphonomycin). In later work at Merck, Dr. Christensen’s focus was in the area of ß-lactam antibiotics. The total syntheses of the penicillins, cephalosporins, cephamycins and carbapenems (especially thienamycin) were all completed at Merck under his direction. The commercial products, Mefoxin® (cefoxitin) and Primaxin® (imipenem, cilastatin), resulted from this research. As part of the nuclear analog program, oxacephalosporins, carbacephalosporins and 1α-methylcarbapenems were first synthesized at Merck.
Groups reporting to Dr. Christensen have also synthesized ivermectin (Ivomec®), the world's largest selling animal health product, PedvaxHIB®, a conjugate vaccine for the prevention of H. influenza and Proscar® (finasteride), a 5α-reductase inhibitor for the treatment of benign prostatic hypertrophy. Several other products in the immunology, antimicrobial, cardiovascular and respiratory areas also entered development.
After taking early retirement from Merck in July, 1992, he became a member of the Scientific Advisory Boards of Microcide Pharmaceuticals, Neurocrine Biosciences, Onyx Pharmaceuticals, Pharmacopeia and Aurora Biosciences and also served as a consultant for Amgen and Genetics Institute. He then co-founded and assumed a full-time position as Executive Vice President, Research, of Advanced Medicine, Inc. (now Theravance, Inc.) During his tenure there, Televancin®, a gram-positive antibacterial agent now awaiting world-wide approval, was synthesized and several other products have since demonstrated efficacy in clinical trials.
He is currently a consultant for Theravance, Inc., Vitae Pharmaceuticals, PharmacoFore, Achaogen, Ensemble Discovery Corp. and Genentech. In 2004, he also served as interim Chief Scientific Officer of Infinity Pharmaceuticals, Inc. during the search for a permanent CSO.
Dr. Christensen has been invited to deliver plenary lectures at over 50 International Symposia and is author of 79 scientific papers and 181 issued U.S. Patents. He also serves on the editorial advisory boards of Medicinal Chemistry and the Journal of Antibiotics. He delivered the Sixth Cecile L. Brown lecture (1974-NJACS) and received the Thomas Alva Edison Patent Award (1985), Merck Directors Scientific Award (1987), Chemical Pioneers Award (1989-AIC) and was elected a Fellow of the AAAS (1996). He also served on the visiting committees of both the Harvard and MIT chemistry departments.
James K. Coward, Ph.D. is Professor of Medicinal Chemistry and Professor of Chemistry, University of Michigan. He obtained the A.B. degree with a major in chemistry from Middlebury College in 1960, after which he was employed as a chemist by American Cyanamid Co. in Stamford, CT. He returned to school at Duke University, intending to pursue a Ph.D. in physical organic chemistry. Following a stimulating introduction to biochemistry by Prof. Philip Handler, he moved to the State University of New York at Buffalo to study medicinal chemistry with Prof. B. R. Baker (Ph.D., 1967). Postdoctoral research in bioorganic chemistry with Prof. Thomas C. Bruice at the University of California, Santa Barbara, supported by a NIH fellowship, completed his formal education at an exciting time when the fields of medicinal chemistry and mechanistic enzymology could interact in a synergistic manner.
In 1969, Coward joined the faculty of the Department of Pharmacology at Yale University School of Medicine. In 1979, he moved to the Department of Chemistry, Rensselaer Polytechnic Institute and in 1987, accepted his present position at the University of Michigan. Initial research involved mechanistic studies of catechol O-methyltransferase and related model reactions. This research was expanded to include the related alkyl transfer reactions catalyzed by spermidine synthase and spermine synthase, two key steps in polyamine biosynthesis. In addition to steady-state kinetic studies, this research involved the use of chiral methyl and methylene substrates to determine the stereochemistry of enzyme-catalyzed alkyl transfer reactions. First-generation inhibitor synthesis focused on metabolically stable analogs of the products, S-adenosylhomocysteine and methylthioadenosine. Second-generation inhibitor synthesis was aimed at “multisubstrate adduct” inhibitors of catechol O-methyltransferase, spermidine synthase (AdoDATO, AdoSpd), and spermine synthase (AdoDATAD). In related research, a series of α-methyl polyamines, designed to resist oxidative metabolism, proved to be useful for the study of polyamine function in vivo.
The biosynthesis and hydrolysis of poly-γ-glutamate derivatives of reduced folates and antifolates are catalyzed by folylpoly-γ-glutamate synthetase, an ATP-dependent ligase, and γ-glutamyl hydrolase, a cysteine peptidase, respectively. Mechanistic research on the synthetase included demonstration of a transient acyl phosphate intermediate using 17O- and 18O-labeled substrates, and kinetic studies on multiple ligations using substrate trapping and pulse-chase methods. Development of a new fluorescence assay for the hydrolase led to an extensive kinetics analysis of enzyme-catalyzed isopeptide hydrolysis. Based on these mechanistic studies, the design and synthesis of a series of phosphinic acid-containing pseudopeptides resulted in potent and specific inhibitors of the synthetase, and methods for the synthesis of internal epoxide peptidomimetics as potential inhibitors of the hydrolase were developed. Extension of this approach has resulted in the synthesis of aryl phosphinic acids as potential inhibitors of dihydrofolate synthetase, a new target for antimalarial drug design, and alkyl phosphinic acids as potent inhibitors of glutathionylspermidine synthetase, a new target for antitrypanosomal drug design.
In the area of carbohydrate chemistry, the Coward group has investigated several glycosyltransferases, including oligosaccharyltransferase. Use of isotopically labeled peptides and disaccharides, as well as developing an epoxide fluoridolysis method for the synthesis of 5-fluoro 2-amino sugars have provided mechanistic insight and inhibitors for this important group of enzymes.
Coward has served the medicinal chemistry community in a variety of leadership positions. He was a member of the Long Range Planning Committee, ACS Division of Medicinal Chemistry (1989-1991) and Alternate Councilor and member of the Executive Committee, ACS Division of Biological Chemistry as (1991-1993). He has served on the Editorial Boards of Biochemical Pharmacology (1984-1996), Journal of Medicinal Chemistry (1988-1992) and Annual Review of Pharmacology & Toxicology (1997-2002). At the University of Michigan, he was the Program Director of the Chemistry-Biology Interface Training Program (1995-2005) and Principal Investigator of the underlying NIH Training Grant. He was the first Chair of a newly created Department of Medicinal Chemistry at the University of Michigan (1998-2004) and Director of the longstanding Interdepartmental Program in Medicinal Chemistry Program during that period. As a member of NIH study sections (Medicinal Chemistry ‘A’, 1979; Experimental Therapeutics, 1979-1982) and review committees (Pharmacological Sciences Review Committee (1987-1991), and numerous advisory panels (NIH, NSF), he has been an advocate for academic medicinal chemistry research. He has been mentor for over 50 graduate students and postdoctoral associates, as well as over 25 undergraduate students. He is a Fellow, Chemistry Section, American Association for the Advancement of Science (2002).
Dr. Robert Vince is a Professor of Medicinal Chemistry at the University of Minnesota. He obtained a B.S. degree in Pharmacy in 1962 and a Ph.D. Degree in Medicinal Chemistry in 1966, both from the College of Pharmacy at SUNY Buffalo. For his graduate research he received the Lunsford Richardson Research Award by Richardson-Merrell Inc. From 1966 to 1967 he was an Assistant Professor of Medicinal Chemistry at the University of Mississippi and in 1967 he joined the Medicinal Chemistry Faculty at the University of Minnesota, where he has been ever since. In 2002 he became the Director of the Center for Drug Design within the Academic Health Center of the University of Minnesota. He has been honored for his work by a career development award from NIH (1972-1976), was the 1979 University of Minnesota Scholar of the year, and received a Certificate of Commendation by the Minnesota Governor (1989). in recognition of achievements as an inventor, was honored for outstanding contributions to research and development by the Minnesota Medical Alley, was elected as Fellow of the AAAS (2000), and received the Outstanding Alumni Award of the New York Cayuga Community College (2002). During President Bush’s 2002 visit to Minneapolis, Robert Vince was selected to speak with him about his research and inventions. He was recognized on “Scholars Walk and Wall of Discovery” at the University of Minnesota in 2006.
Professor Vince’s scientific contributions and eclectic approach to solving problems have focused on unique approaches to the development of novel chemotherapeutic agents. He has co-authored over 110 scientific publications and holds 23 patents. His research was funded by the National Cancer Institute without interruption from 1971 to 1998, when Professor Vince was able to fund his research from licensing income. It is highly unusual for a drug candidate from an academic laboratory to make it through the extremely competitive pharmaceutical drug development process to the point of becoming a new drug. Professor Vince was involved in it twice. The drug, AcyclovirTM, that has been the standard treatment for Herpes infections, is a member of the acyclonucleoside family pioneered by Robert Vince and Professor Howard J. Schaeffer at SUNY Buffalo. Professor Vince's most notable achievement, however, is his design of the carbocyclic nucleosides termed "carbovirs", agents that were later developed into the anti-HIV drug, ZiagenTM that is marketed worldwide by GlaxoSmithKline for the treatment of AIDS in adults and children. The carbovirs were the first series of agents that showed significant activity against the human immunodeficiency virus (HIV) and Hepatitis B Virus. In 1987, the National Cancer Institute Decision Network Committee for Preclinical Development (chaired by Dr. Bruce Chabner), selected the carbovirs, the first of the anti-HIV compounds that were specifically designed for inhibiting the AIDS virus, for accelerated preclinical development. The University of Minnesota (UM) licensed the carbovir drugs to Glaxo Pharmaceutical Company in 1988. However, due to circumstances beyond the control of the University of Minnesota, the development of the drug was delayed and did not make it to market until 1998. This discovery has led to sixteen U.S. patents and several foreign patents. Sales of the drug continue to rise with last year's sales exceeding $850,000,000. The starting chemical for the production of this drug and other carbocyclic nucleosides was developed by Professor Vince's laboratory in the late 1970's. This material, referred to as "Vince's Lactam" is produced in metric ton quantities by several chemical companies.
The impact on science education is a secondary benefit to Professor Vince’s invention. The University of Minnesota has received approximately 250 million dollars in royalties from GlaxoSmithKline from worldwide sales of ZiagenTM. A large part of these royalties were used by the University to set up the Strategic Research Fund, the Strategic Research Endowment, the Graduate Fellowship fund, and the Graduate Fellowship Endowment, as well as the Robert Vince Endowed Chair. The University has also supported Dr. Vince's creation of the Center for Drug Design that provides positions for faculty and fellowships for graduate students and postdoctoral fellows. The Center provides an excellent collaborative research environment, and has state-of-the-art medicinal chemistry research and drug development capabilities.
For 35 years Professor Vince has taught medicinal chemistry to undergraduate pharmacy students, medicinal chemistry graduate students and postdocs at the University of Minnesota. He has advised a large number of doctoral and postdoctoral students in his laboratory, who have gone on to very productive careers. Professor Vince has served on various committees within the College of Pharmacy, and the University of Minnesota, where he helped shape university policy on intellectual property and royalty distribution. He served on various study sections of the National Institute of Health, serves on the editorial board for Nucleosides and Nucleotides, and has been a consultant to the pharmaceutical industry. Professor Robert Vince has combined excellence in research and teaching by carrying out outstanding medicinal chemistry research and by training several generations of students to become excellent scientists in their own rights. He has succeeded in doing what very few academic scientists and not many industrial scientists accomplish, and royalty income from his inventions has enabled the creation of a Center for Drug Design at the University of Minnesota that has already gained international reputation for excellence in medicinal chemistry research.
Adjunct Senior Research Chemist at Columbia University working in the laboratory of Professors Koji Nakanishi and Nina Berova
George obtained a BS and MS in chemistry from Oregon State University in 1957 and 1958 and a PhD in organic chemistry from UCLA in 1962. After postdoctoral studies at the University of London he joined Lederle Laboratories in Pearl River, New York in1964.
His almost 40- year career at Lederle/Wyeth included structural and bioorganic studies on pharmacologically active mold metabolites; spermidine, glycopeptide and tetracycline antibiotics; enediyne antitumor agents; and finally biophysical chemistry and enzymology for hit and lead characterization and assay development. His group’s efforts on the structure and DNA cleavage chemistry of the enediyne antitumor agent calicheamicin help lead to Mylotarg®, an antibody conjugate for use in the treatment of acute myologenous leukemia in elderly patients shown to be refractory to conventional chemotherapy.
He also contributed to the development of Tygacil®, a new semisynthetic tetracycline active against resistant bacterial infections that are no long susceptible to previously useful antimicrobial agents. George retired from Wyeth in 2004 and in 2005 became an Adjunct Senior Research Chemist at Columbia University working in the laboratory of Professors Koji Nakanishi and Nina Berova.
Dr. Gary Grunewald is a Professor of Medicinal Chemistry at the University of Kansas. He obtained undergraduate degrees in both chemistry and pharmacy at Washington State University where he was elected to membership in Phi Beta Kappa. He received a Wisconsin Alumni Research Foundation Fellowship and an NIH Predoctoral Fellowship for his graduate work at the University of Wisconsin. His Ph.D. dissertation (with Howard Zimmerman) described the chemistry of barrelene and included the photochemical conversion of barrelene to semibullvalene, the first recognized example of the di-p-methane rearrangement. He then joined (1966) the faculty at the University of Kansas in the Department of Medicinal Chemistry where he has been ever since. He served as department chair in 1994-2003. He received the Higuchi/Simons Research Achievement Award for research excellence in the biomedical sciences at the University of Kansas. His research has concentrated on mechanistic studies of neurotransmitters and drugs affecting them in the central nervous system employing most of the techniques of drug design (conformationally defined (rigid) analogs, QSAR, molecular modeling, site-directed mutagenesis and structure-based drug design using protein crystallography). He has had the good fortune of working with a number of excellent senior collaborators and with a wonderful group of undergraduate, graduate and postdoctoral students. In studies of conformation-activity relationships his group showed that that amphetamine had one optimal conformation for inhibition of the reuptake of catecholamine neurotransmitters but had a different optimal conformation for causing vesicular release of the same neurotransmitter in presynaptic neurons. His group was able to explain why homozimeldine retained the selectivity for the serotonin transporter over the norepinephrine transporter that its parent zimeldine displayed and also explained, through molecular mechanics calculations, why homozimeldine was less potent than the parent zimeldine. Recent work has concentrated on finding a potent and selective inhibitor of epinephrine biosynthesis to explore the poorly understood role of epinephrine in the central nervous system. Through use of rigid analogs they showed that phenylethylamines bind to the enzyme in a fully extended conformation and they confirmed the reality of this conclusion using transferred nuclear Overhauser enhancements to determine the torsion angles of the flexible ligand 3,4-dichloroamphetamine when bound to the enzyme. They have shown that a careful combination of steric factors and pKa control using ß-fluorination (an example of the Goldilocks Effect) can result in a potent inhibitor of phenylethanolamine N-methyltransferase that shows extremely low affinity for the competing binding site, the α2-adrenoceptor. Through a combination of nmr studies and quantum chemical calculations, they were able to accurately predict the relative stereochemistry of six of the seven chiral centers in epothilone before the x-ray crystal structure of this anticancer drug was known.
He has served the Medicinal Chemistry Division of ACS as a member of the Long Range Planning Committee (1991-1994), as Vice Chair (1993), Chair (1994) and Councilor (1999-2001). He served as general chair of the 27th National Medicinal Chemistry Symposium in 2000. He served as Chair of the Research Committee (1983-85) and as a member of the Board of Directors (1980-1991) of the Kansas Affiliate of the American Heart Association He also served as Chair of the Medicinal Chemistry and Pharmacognosy Section of the Academy of Pharmaceutical Sciences (1983) and as Chair of the Pharmaceutical Sciences Section of the American Association for the Advancement of Science (1994). He serves on the Editorial Advisory Boards for Bioorganic and Medicinal Chemistry and Bioorganic and Medicinal Chemistry Letters. He was elected as a Fellow of both the AAPS (2006) and AAAS (1992).
30 years of experience in discovering and developing drugs at Merck Research Laboratories
Joel R. Huff has 30 years of experience in discovering and developing drugs at Merck Research Laboratories. He initially joined Merck as a senior research chemist and was subsequently promoted to positions of increasing responsibility, resulting in his appointment to Vice President of Medicinal Chemistry in 1994. Dr. Huff retired from Merck in 2004. During his tenure at Merck, he led efforts to develop therapeutic agents for HIV that resulted in the discovery of indianvir (Crixivan®), and efavirenz (Stocrin®, Sustiva®). Dr. Huff has authored or co-authored 98 publications and patents. He has been the recipient of various awards including the Merck Board of Directors Award (1998), the Pharmaceutical Research and Manufacturers of America Discoverer's Award (1999), the ACS Philadelphia Section Award (2002), the ACS Alfred Burger Award in Medicinal Chemistry (2006), and induction into the ACS Division of Medicinal Chemistry Hall of Fame (2007). He holds a B.S. in Chemistry from the University of Texas, Austin, TX., and a Ph.D. in Organic Chemistry from the Massachusetts Institute of Technology.
Dr.William F. Michne was born in Albany, New York, on December 9, 1942, the youngest of three children. His father was a welder in the repair shops of the New York Central Railroad, and his mother was a part-time waitress. He received a Bachelor degree in chemistry from Siena College in 1964, and began immediate employment at the Sterling-Winthrop Research Institute as an Assistant Research Chemist. Simultaneously, he began graduate studies in organic chemistry at Rensselaer Polytechnic Institute, earning a doctorate in 1968.
His first major scientific achievement was the synthesis of a series of benzomorphanones. These analogs of the opiate alkaloid morphine exhibited unusual pharmacological properties, both in vitro and in vivo, relative to all previously studied compounds in this class. While they were very potent in assays for morphine-like behavior, their activity was rather insensitive to reversal by naloxone, a morphine antagonist. Further study of one of these compounds, ketazocine, led to the discovery of the kappa opioid receptor subtype. Ketazocine advanced to human clinical trials for pain. The single enantiomer ethylketazocine, more commonly known as EKC, advanced to preclinical development as an intravenous anesthetic, and was widely used in early studies of the kappa receptor.
The next major phase of his career extended his work on benzomorphans to analogs of the exceedingly potent opiates known as thebaine Diels-Alder adducts. He and his co-workers devised a stereospecific synthesis of a very challenging construct of three contiguous asymmetric centers two of which were adjacent and quaternary. The synthesis was eventually carried out on multi-kilogram scale to support the advancement of three compounds. One of them, tonazocine, was the first non-peptide delta opioid agonist, and was clinically as efficacious as morphine.
Over the next decade his career advanced with positions of increasing responsibilities. Research groups under his direction had highly focused programs in the areas of pain and inflammation, cardiovascular agents, anti-viral agents, and immunology. During this time period these groups produced two compounds in clinical evaluation, an additional three compounds in advanced safety evaluation, a total of twenty-three patents, thirty-two publications, and twenty-six presentations.
The early nineties saw the emergence of high-throughput screening, with the attendant problem of how to sort through the huge amounts of data being generated to find the compounds or series most likely to advance through the development process. He took up this challenge, and with a half dozen or so co-workers developed the objectives necessary to quickly achieve this goal. He published the first description of the Hit-to-Lead process as a stand alone concept in 1996, setting forth the five objectives of Hit-to-Lead that remain valid today, despite the more recent addition of further optional components that can increase the value of this separate phase.
In 1994 he joined Astra, which became AstraZeneca. He was Director of Chemistry at the Rochester, NY site, then at the Worcester, MA site. During the last five years of active employment, he assumed the position of Senior Principal Scientist at the Wilmington, DE site. Here he began to address fundamental questions of small molecule biological activity and selectivity. His work in this area continues with academic collaborators.
Throughout his career he was very active in the external scientific community. As an Associate Professor of Chemistry at the Albany College of Pharmacy he taught medicinal chemistry for seven years. He has served on the editorial advisory board of the Journal of Medicinal Chemistry, and was a section editor for Annual Reports in Medicinal Chemistry. He served on the ACS Medicinal Chemistry Division Long Range Planning Committee, and has organized several meeting symposia. He was Chair of the 1999 Gordon Conference on Medicinal Chemistry, and Co-Chair of the 2002 National Medicinal Chemistry Symposium. He was also Co-Chair of the Conference on New Chemical Technologies Accelerating Drug Discovery, 2001, and served on the Advisory Board for Hit-to-Lead, World Pharmaceutical Congress, 2004.
Dr. William J. Greenlee was born in 1950 in Columbus, Ohio. He began his career in chemistry as a high school student while working at his father’s company, “Chemical Samples Company,” synthesizing and purifying acetylenes and other hydrocarbons. While an undergraduate at The Ohio State University, Greenlee carried out research with Prof. Paul Gassman on strained ring hydrocarbons. After receiving his B.S. degree in chemistry at OSU in 1972, Greenlee was awarded an NSF Predoctoral Fellowship and carried out graduate studies with Prof. Robert B. Woodward at Harvard University. He received his Ph.D. degree from Harvard in 1976, after completing the first total synthesis of (+/-)-Marasmic acid. He was an NIH Posdoctoral Fellow at Columbia University with Prof. Gilbert Stork, and was a member of the team that completed the first total synthesis of Cytochalasin B.
Dr. Greenlee joined Merck Research Laboratories in 1977 as a member of the New Lead Discovery department where he became part of the Merck team under Dr. Arthur Patchett that discovered potent inhibitors of angiotensin-converting enzyme, including enalapril (Vasotec™) and lisinopril (Prinivil™). Greenlee and his group also worked on angiotensin II receptor antagonists, an effort that evolved into a collaboration with scientists at the Dupont Merck Pharmaceutical Company. Greenlee’s team identified several potent angiotensin AT1 antagonists including MK-996, and developed the first potent dual AT1/AT2 antagonists. His group also discovered potent angiotensin AT1 agonists, the first nonpeptide agonists of a peptide receptor outside the opioid field. He and his associates also developed potent renin inhibitors and endothelin receptor antagonists. He was promoted to Director in 1989 and to Senior Director in 1992.
In 1995, Greenlee joined the Schering Plough Research Institute (SPRI) as Senior Director, Cardiovascular and CNS Chemical Research, and was promoted in 2002 to Vice President, CNS and Cardiovascular Chemistry and High-Throughput Synthesis. At Schering-Plough, he directed a group of 80 chemists in the design and synthesis of potential drug candidates for treatment of Alzheimer’s disease, obesity, diabetes, thrombosis and chronic pain. His group discovered ten development candidates that have entered clinical trials. Following the acquisition of Schering-Plough by Merck in 2009, Greenlee served as Chemistry Site Head in Kenilworth, and then returned to Rahway as Senior Director of Medicinal Chemistry in 2010. Since November, 2011, he has been working as an independent consultant in medicinal chemistry and drug discovery.
Greenlee chaired the Medicinal Chemistry Gordon Conference in 1997 and served as Chair and Program Chair for both the Medicinal Chemistry (2003) and Organic Chemistry (2004) Divisions of the American Chemical Society. He is currently serving his second term as Councilor for the MEDI Division. He served as Section Editor (Cardiovascular and Pulmonary), for Annual Reports in Medicinal Chemistry (1999–2004), and is currently Perspectives Editor for the Journal of Medicinal Chemistry. He and is a member of the Editorial Advisory Board for ACS Medicinal Chemistry Letters, and is Co-Organizer of the annual Drew University Residential School on Medicinal Chemistry. Greenlee received the Alfred Burger Award in Medicinal Chemistry from the American Chemical Society in 2004. He was elected a Fellow of the American Association for the Advancement of Science in 2007 and an ACS Fellow in 2009. He is author of more than 180 research publications and inventor of over 60 U.S. patents.
Christopher A. Lipinski earned the B.S. degree in chemistry at San Francisco State College and a Ph.D. in physical organic chemistry at the University of California, Berkeley. Following postdoctoral work at California Institute of Technology, he joined Pfizer in 1970. His 1997 publication of the "Rule of Five" is a landmark paper in the medicinal chemistry literature. He has served on a number of Advisory Boards and Editorial Boards. He has over 190 publications and holds 17 US patents.
Dr. Lipinski was the 2004 recipient of the ACS Division of Medicinal Chemistry Award, and the 2005 recipient of the E.B. Hershberg Award for Important Discoveries in Medicinally Active Substances.
Solon E. Summerfield Distinguished Professor of Pharmaceutical Chemistry at The University of Kansas- Lawrence
Ronald T. Borchardt is the Solon E. Summerfield Distinguished Professor of Pharmaceutical Chemistry at The University of Kansas- Lawrence. Professor Borchardt received his undergraduate education (B.S. in Pharmacy, 1967) from the University of Wisconsin-Madison and his graduate education (Ph.D. in Medicinal Chemistry, 1970) from The University of Kansas-Lawrence. After serving as a Postdoctoral Fellow at the National Institutes of Health (Bethesda, Maryland) from 1969-1971, Professor Borchardt returned to The University of Kansas as an Assistant Professor. In the 1970's Professor Borchardt was promoted through the academic ranks to his current position as Solon E. Summerfield Distinguished Professor. From 1983-1998, Professor Borchardt served as the Chairman of the Department of Pharmaceutical Chemistry in the School of Pharmacy at The University of Kansas. During his academic career, Professor Borchardt supervised the research of approx. 170 graduate students, postdoctoral fellows and visiting scientists.
Professor Borchardt’s research interests include both drug delivery and drug design. In the area of drug delivery, his interests include: (i) the development of epithelial and endothelial cell culture systems for the study of drug transport and metabolism; (ii) the development of rational strategies (e.g. prodrugs) to improve the transport characteristics of peptides and peptidomimetics; (iii) the elucidation of the chemical pathways of protein and peptide degradation; and (v) the development of strategies to stabilize biomolecules in pharmaceutical formulations. Professor Borchardt’s interest in drug design has focused on the design and synthesis of inhibitors of an enzyme (S-adenosylhomocysteine hydrolase) that plays a key role in regulating biological methylation reactions, which are crucial for the replication of some viruses and parasites.
Professor Borchardt contributions to the development and validation of cell cultures for studying drug transport across the intestinal mucosa and the blood-brain barrier have been particularly significant. His pioneering work in the late 1980s lead to the introducing of Caco-2 cells as a model of the intestinal mucosa. This cell culture model is now widely used by scientists in pharmaceutical/biotechnology companies and in academic and government laboratories worldwide. Based upon his medicinal chemistry background, Professor Borchardt has more recently utilized this in vitro cell culture model for studying how structure influences transport of drugs across the intestinal mucosa.
During his academic career Professor Borchardt has received numerous awards and honors for his teaching and research accomplishments including: Established Investigator from the American Heart Association (1974-1979); Sato Memorial International Award from the Pharmaceutical Society of Japan (1981); Mortar Board Outstanding Educator Award (1980), Dolph C. Simons, Sr. Research Award in the Biomedical Sciences (1983), the Louise Byrd Graduate Educator Award (1997) and the Chancellors Club Career Teaching Award (2005) from The University of Kansas; Fellow of the American Association of Pharmaceutical Scientists (1988) and the American Association for the Advancement of Science (1995); Citation of Merit from the University of Wisconsin (1989); Meritorious Manuscript Awards (1991, 1998), Research Achievement Awards in Biotechnology (1993) and Medicinal Chemistry (1994), and Distinguished Pharmaceutical Scientist Award (1997) from the American Association of Pharmaceutical Scientists; Takeru and Aya Higuchi Memorial Lectureship Award from the Academy of Pharmaceutical Sciences and Technology of Japan (1993); Paul Dawson Biotechnology Award (1997) and Volwiler Research Achievement Award (1998) from the American Association of Colleges of Pharmacy; Hoest-Madsen Medal (1999) from the International Pharmaceutical Federation; Distinguished Service Award (1999) from the FASEB Research Conference on Biological Methylation; the Millennial Pharmaceutical Scientist Award (2000) from the Millennial World Congress of Pharmaceutical Sciences; the Research Achievement Award in the Pharmaceutical Sciences (2001) and the Takeru Higuchi Research Prize (2003) from the American Pharmaceutical Association; the Smissman-Bristol-Myers Squibb Award from the Medicinal Chemistry Division of the American Chemical Society (2003); PolyPops Foundation Award from the Society for Biomolecular Sciences (2007); and Honorary Doctorate Degrees from The Danish University of Pharmaceutical Sciences, Copenhagen, Denmark (2002), Katholieke University, Leuven, Belgium (2004) and Uppsala University, Uppsala, Sweden (2006).
Professor Borchardt is the author or co-author of approximately 495 scientific publications and 460 abstracts. He is also the Editor of 10 books, and the Series Editor of "Pharmaceutical Biotechnology" (14 published volumes, Springer) and “Biotechnology: Pharmaceutical Aspects” (7 published volumes, AAPS Press/Springer).
Distinguished Research Professor of Chemistry & Co-Director in the Department of Chemistry & Chemical Biology at the Stevens Institute of Technology, Hoboken, NJ
Born in India, Prof. A.K.Ganguly earned his undergraduate and master’s degrees in chemistry from Delhi University, where he also completed his Ph.D. in organic chemistry in 1959 under the supervision of Prof. T.R.Seshadri. As a testament to his high level of scholarship, he then received the prestigious 1851 Exhibition Scholarship, awarded annually by the Royal Commission, Great Britain, to only one student of science from India to study in England. He attended the Imperial College of Science and Technology, London, where he obtained his second Ph.D. in chemistry in 1961. There, he studied under the supervision of Sir Derek Barton, a Nobel Laureate in chemistry, whom Dr. Ganguly credits as the greatest influence of his scientific career.
After finishing his studies at the Imperial College of Science and Technology Prof. Ganguly returned to India to work for Glaxo Laboratories in Bombay. After a brief period of stay at Glaxo he moved to the Ciba Research Center, also in Bombay, where he established a fruitful collaboration with Prof. T.R.Govindachari.
Prof Ganguly immigrated to the United States in 1967 and worked with Sir Derek at the Research Institute of Medicine and Chemistry, Cambridge, Massachusetts before joining the Schering-Plough Research Institute, Kenilworth, NJ in 1968 as a Senior Scientist. At Schering-Plough Research Institute he progressed to the position of Senior Vice President of Chemical Research in which capacity he directed all aspects of Chemical Research at the institute. In September 1999 he joined Stevens Institute of Technology, Hoboken, NJ where he is presently a Distinguished Research Professor of Chemistry and Co-Director in the Department of Chemistry and Chemical Biology. He teaches Medicinal Chemistry and directs research programs for graduate students at Stevens.
Prof. Ganguly has made many significant contributions in drug discovery. He is associated with the discoveries of Ezetimibe (Zetia), a cholesterol absorption inhibitor; Noxafil (Posaconazole), a potent antifungal; Lonafarnib (Sarasar), a highly selective farnesyl protein transferase inhibitor for the treatment of cancer and SCH 503034, an orally active inhibitor of Hepatitis C Virus protease. Prof. Ganguly is also recognised for his many contributions towards synthesis of other biologically active molecules. In the area of infectious diseases, Prof. Ganguly’s contribution towards solving the very complex structure of Ziracin, a potent antibiotic which is active against Methicillin resistant Staph. aureus and synthesis of Penem antibiotics are widely recognized in the scientific community.
Prof. Ganguly has published two hundred thirteen papers and is a co inventor of eighty-seven patents, and has been a plenary lecturer at many international meetings. He has received several awards, a partial list of which is shown below:
1. Recipient of Professor Seshadri Memorial Award for the year 1982.
2. Charles Sabat Lecturer, Rutgers University, 1987.
3 Recipient of "Outstanding Scientist Award" given by the Association of Scientists of Indian Origin in America, Inc., 1991.
4. Third Herman S. Bloch Memorial Lecturer at The University of Chicago, 1995.
5. Ranbaxy Science Foundation Award for Pharmaceutical Sciences, 1997.
6.. Gurbax Singh Memorial Award Lecture for Biomedical Sciences, 1999.
7. E. B. Hershberg Award for important discoveries in medicinally active substances, American Chemical Society, 2003.
8. Presidential Lecture at the Acadia University, Canada, 2003.
9. Doctor of Engineering (Honoris Causa) from Stevens Institute of Technology, 2004.
10. Lifetime achievement award, Indian Chemical Society, 2004
11. Thomas Alva Edison Award, 2006
12. Hall of Fame, Medicinal Chemistry, American Chemical Society, 2007.
Prof. Ganguly remains as a consultant at Schering-Plough Research Institute .
Director of the Center for Organic & Medicinal Chemistry & a Distinguished Fellow for Medicinal Chemistry
Dr. F. Ivy Carroll received the B.S. degree in chemistry from Auburn University in 1957 and was awarded the Ph.D. in chemistry by the University of North Carolina at Chapel Hill in 1961. He joined the research staff of the Research Triangle Institute as a Research Chemist and rose steadily to the position of Vice President of the Chemistry and Life Sciences Group, a position he held from 1996 to 2001. Dr. Carroll is presently Director of the Center for Organic and Medicinal Chemistry, a position he held since 1975, and is a Distinguished Fellow for Medicinal Chemistry (a position equivalent to Vice President).
Dr. Carroll is a member of the American Chemical Society (ACS); a fellow of the American Association for the Advancement of Science (AAAS), the American Association of Pharmaceutical Science (AAPS), the Royal Society of Chemistry (RSC), and the College on Problems of Drug Dependence (CPDD); and the honor societies, Sigma Xi and Phi Lambda Upsilon. His other professional and scientific activities include service on the Long-Range Planning Committee of the Medicinal Chemistry Section of the ACS and two terms of service on the ACS Offices and Awards Committee (Chairman for the last term). Dr. Carroll was a member of the Biochemistry Study Section of the National Institute on Drug Abuse Review Committee for four years; a member of the Molecular, Cellular, and Chemical Neurobiology Research Review Committee for two years; and a member of the Medications Development Division Review Committee of the National Institute on Drug Abuse for four years (Chairman for two years). He is presently a member of the NIH Molecular Neuropharmacology and Signaling Study Section. Dr. Carroll served on the Editorial Advisory Board of the Journal of Medicinal Chemistry from 1995 to 1999. He is presently the Medicinal Chemistry Section Editor for Drug Development Research, and is on the advisory boards of several other journals.
Dr. Carroll has made significant contributions to anti-cancer, anti-radiation, and anti-malarial research; however, his more recent studies have been directed mainly to drug abuse and central nervous system research. A major thrust of his research has involved the synthesis and pharmacological characterization of the 3-phenyltropane class of compounds. These compounds have had tremendous impact as tools to assist in establishing the biochemical mechanism of action of cocaine. The longer-term goal of this research was the identification and development of treatment drugs for cocaine addiction. This effort identified the dopamine transporter-selective analog, 3ß-(4'-chlorophenyl)-2ß-[3-(4’-methylphenyl)isoxazol-5-yl]tropane (RTI-336), as a pharmacotherapy for treatment of cocaine abuse. Preclinical studies have been completed, and the IND will be submitted in early 2008.
The 3-phenyltropane research has also led to the development of 3ß-(4-iodophenyl)tropane-2ß-carboxylic acid methyl ester (RTI-55). The radioisotopically labeled forms of RTI-55 have found commercial applications. [125I]RTI-55 is highly useful for biochemical studies of monoamine transporters and is presently marketed by Perkin Elmer. [123I]RTI-55 (Dopascan, Iometopane), also developed by Dr. Carroll, is a single photon emission computed tomography (SPECT) imaging ligand used as a diagnostic agent for Parkinson's disease. Thousands of patients have been diagnosed in the US, European countries, Japan, Korea, Taiwan, and Scandinavian countries. [123I]RTI-55 has also been heavily used as a clinical tool to study drug abuse patients. Dr. Carroll has 22 publications and seven patents devoted solely to RTI-55.
Dr. Carroll’s more recent research has been directed toward the study of opioid and nicotinic receptors. Most significantly, the studies have discovered JDTic, a potent and kappa opioid receptor selective antagonist. JDTic is the only small molecule kappa opioid selective antagonist not derived from the morphine-like structure, and JDTic is the only orally active kappa opioid receptor antagonist. Orally administered JDTic is active in the stress-induced cocaine relapse rat model and is also active in the rat forced-swim anti-depression model and in anxiolytic tests in rats. Preclinical studies are well on the way for IND submission for JDTic. In addition, Dr. Carroll’s opioid receptor research has lead to the development of four new structural types of opioid receptor pure antagonists, new structural types of opioid inverse agonists, and a novel structural type of opioid agonist.
The nicotinic research has provided [125I]iodo-MLA, which is the most selective ?7-nicotine receptor radioligand presently available, and 2-fluoro-(4-nitrophenyl)deschloro¬epibatidine (4-nitro-PFEB), which is the most potent and α4ß2 selective, competitive antagonist presently available. A number of other compounds have also been developed that serve as pharmacological tools to characterize the behavioral properties resulting from interaction with nicotinic receptors. Dr. Carroll's research efforts showed that (2S,3S)-hydroxybupropion, a major bupropion metabolite, is an α4ß2 AChR antagonist and, thus, may contribute to bupropion’s smoking cessation activity.
Dr. Carroll's research is documented in 393 peer-reviewed publications, 32 book chapters, and 36 patents. Ninety postdoctoral fellows have been trained by Dr. Carroll.
Awards and honors recognizing Dr. Carroll’s research accomplishments include: the 1993 Distinguished Lecturer award from the North Carolina Section of the American Chemical Society, the 2000 Southern Chemist Award from the Memphis Section of the American Chemical Society, the 2001 Herty Award from the Georgia Section of the American Chemical Society, the 2002 American Chemical Society Medicinal Chemistry Award, the Research Triangle Institute 2001 Margaret E. Knox Excellence Award, the 2006 Nathan B. Eddy Award from the College on Problems of Drug Dependence, and the 2006 Research Achievement Award in Drug Design and Discovery from the American Association of Pharmaceutical Scientists. The National Institute on Drug Abuse honored Dr. Carroll with the 1993 Pacesetter award and the 1996 MERIT award for his research on the biochemical mechanisms of the action of cocaine.
Founding Director for the Institute of Chemical Biology & Drug Discovery (ICB&DD) at Stony Brook
Professor Iwao Ojima received his B.S. (1968), M.S. (1970), and Ph.D. (1973) degrees from the University of Tokyo, Japan. He joined the Sagami Institute of Chemical Research and held a position as Senior Research Fellow until 1983. He joined the faculty at the Department of Chemistry, State University of New York at Stony Brook first as Associate Professor (1983), was promoted to Professor (1984), Leading Professor (1991), and then to Distinguished Professor (1995). He served as the Department Chairman from1997 to 2003. He serves as the founding Director for the Institute of Chemical Biology & Drug Discovery (ICB&DD) at Stony Brook from 2003. He has been a Visiting Professor at the Université Claude Bernard Lyon I, Lyon, France (1989), The University of Tokyo, Tokyo, Japan (1996), The Scripps Research Institute, La Jolla, CA (1997), and Université de Paris XI, BIOCIS, Châtenay-Malabry, France (1997).
His research interests include drug design and discovery (anticancer agents, antibacterial agents, enzyme inhibitors), medicinal chemistry and chemical biology, catalytic asymmetric synthesis, organic synthesis by means of organometallic reagents and catalysts, peptidomimetics, ß-lactam chemistry, and organofluorine chemistry (fluoroamino acids and peptides, medicinal applications).
He has published more than 350 papers and reviews in leading journals and more than l50 patents and patent applications, edited 6 books (SciFinder lists >640 publications to his credits), and he has given more than 80 Plenary and Invited Lectures in international conferences and symposia by August 2007.
He is a recipient of the Arthur C. Cope Scholar Award (1994) and the E. B. Hershberg Award (for important discovery of medicinally active substances) (2001) from the American Chemical Society; The Chemical Society of Japan Award (for distinguished achievements) (1999) from the Chemical Society of Japan; Outstanding Inventor Award (2002) from the Research Foundation of the State University of New York. He was inducted into the Medicinal Chemistry Hall of Fame, American Chemical Society (2006). He is a Fellow of the J. S. Guggenheim Memorial Foundation (1995-), the American Association for the Advancement of Science (1997-), and The New York Academy of Sciences (2000-).
To describe his contributions to medicinal chemistry, the Chemical & Engineering News wrote as follows on the occasion of his E. B. Hershberg Award in 2001 (excerpt): “Explorers have always faced enormous risks to attain a lifelong ambition. Some explorers risk life and limb going deep under the oceans or deep into space, or by facing human-averse climates and altitudes to reach a spot on Earth rarely if ever seen before. IWAO OJIMA, however, is a different breed of explorer. His tools for exploration are nuclear magnetic resonance, infrared, UV, mass, and fluorescence spectrometers; liquid chromatographs; amino acid sequencers; microscopes; and computer workstations. Ojima, Distinguished Professor and chairman of the department of chemistry at the State University of New York, Stony Brook, has dedicated his life to discovering the microscopic world.
According to one of his colleagues, ‘That Ojima has been able to put down such a large footprint arises from a most unusual mix of abilities that includes organic synthesis, keen insights into good pharmaceutical problems, and the ability to induce people in diverse disciplines to work together toward a common goal.’
Ojima's research includes four areas of intense interest to the pharmaceutical industry: fluorine-containing amino acids, peptides, and enzyme inhibitors; the development of antithrombic agents; the development of novel ß-lactams; and contributions to the development of second- and third-generation taxoids. In the first area, Ojima has been at the forefront in the incorporation of fluoro-amino acids into peptides. His research led to a series of trifluoromethyl-containing enzyme inhibitors and brain peptides.
In the development of antithrombic agents, he has worked on rational modification of the RGD (Arg-Gly-Asp) pharmacophore to develop double-strand RGD peptides as well as RGD peptidomimetics with enhanced antiplatelet activity. His work with ß-lactams, including development of the ß-lactam synthon method, led him to develop efficient and versatile methods for the asymmetric synthesis of ß-hydroxy and ß-amino acids, their derivatives and peptides, diamino and hydroxyamino acids, diamino alcohols, and polyols. But perhaps Ojima's greatest explorations have been his discovery and development of second- and third-generation taxoids, some of which are in clinical trials, and taxane-based multi-drug-resistance (MDR) reversal agents. His group has been central in clarifying the binding mode of Taxol to its receptor tubulin on a 3-D molecular structural basis and also in its interaction with P-glycoprotein, which is responsible for MDR.
A colleague adds that "Ojima has been able to bring new and interesting organic chemistry to bear on the advancement of medicinal chemistry in a big way." The "microscopic" discoveries made by Ojima are saving lives today—that's one giant leap for mankind. …….—ARLENE GOLDBERG-GIST”.
He has served and has been serving in various advisory committees for National Institutes of Health (National Cancer Institute, National Institute of General Medical Sciences), National Science Foundation and the U.S. Department of Energy. He has served as a member of the Executive Committee for the Division of Organic Chemistry and the Long Range Planning Committee for the Division of Medicinal Chemistry, American Chemical Society.
He has also served and has been serving as Editorial Advisory Board member ofJournal of Organic Chemistry, Organometallics, Journal of Molecular Catalysis,Current Topics in Medicinal Chemistry (current), Medicinal Chemistry (current),Letters in Drug Design & Discovery (current), Anti-Cancer Agents in Medicinal Chemistry (current), Bulletin of the Chemical Society of Japan (current), and Anti-Cancer Agents in Medicinal Chemistry (current). He has also served as the Guest Editor for thematic issues of the Journal of Medicinal Chemistry, Accounts of Chemical Research, and Current Topics in Medicinal Chemistry.
He has been active in organizing important symposia such as (a) Symposium on "New Hope for Breast Cancer Chemotherapy" (1993), (b) Symposium on "Recent Advances in the Chemistry of Taxane and Taxoid Anticancer Agents" (1994), (c) Symposium on "Fluoroamino Acids and Peptides in Medicinal Chemistry" (1995), (d) Symposium on “New Prospects in Anticancer Agents for the 21st Century”, the (2000), (e,f,g) Ernest Guenther Award Symposium (2000, 2005, 2007), (h) Symposium on “Drug Resistant Tuberculosis – Challenge in Chemotherapy” (2005), (i) ACS Award in Organometallic Chemistry Symposium (2006), (j) Symposium on “Modern Natural Products Chemistry and Drug Discovery” (2006), (k) Symposium on “Modern Molecular Strategies for Tumor-Targeting Drug Delivery (2007).
Dr. John J. Baldwin received his BS degree in Chemistry in 1956 from the University of Delaware and his Ph.D. Degree at the University of Minnesota. While at Minnesota, he was elected President of Sigma Xi and was recipient of the Outstanding Achievement Award in Organic Chemistry. After graduation, Dr. Baldwin spent over 40 years focused on drug discovery and in exploring new technologies to increase the efficiency of the discovery process. He started his career at the Merck Research Laboratories, leaving after 30 years with several drugs to his credit including Trusopt® and Cosopt®, both for the treatment of glaucoma. While at Merck he made important contributions to a wide range of therapeutic areas including, cardiovascular medicine with Aggrastat®, Aids with Crixivan®, and to peptic ulcer disease where he played a key role in the development of Pepcid®. Dr. Baldwin next became founder and Chief Scientific Officer of Pharmacopeia, a company specializing in new drug discovery technologies. From this work several drugs are currently undergoing clinical investigation. After 10 years at Pharmacopeia, he founded, and is President and Chief Scientific Officer for Vitae Pharmaceuticals where he applies computational and molecular simulation methods to the discovery of new therapeutic agents. Dr. Baldwin has published over 100 scientific articles and numerous reviews and has been an invited lector at more than 125 national and international symposiums. He holds over 180 issued United States patents. He has received several awards in recognition of his work including the prestigious Hershberg Award for Important Discoveries in Medically Active Substance and the Outstanding Achievement Award by the University of Minnesota. He was inducted into the Medicinal Chemistry Division Hall of Fame at the 2007 Fall ACS Meeting. He is a cofounder and member of the Board of Directors of WuXi PharmaTech in Shanghai, China; he also serves on the Board of Directors of GlycoMimetics and Glyconix Corporations.
Professor of Medicinal Chemistry in the College of Pharmacy at The University of Michigan
Dr. John G. Topliss was born near Mansfield, England in 1930. He received a BSc degree with honors in chemistry, first class, in 1951 from The University of Nottingham and a Ph.D. degree in organic chemistry with Professor F. E. King on the total synthesis of tricyclic diterpenoids from the same institution in 1954. He then did postdoctoral research with Professor Holger Erdtman at The Royal Technical College in Stockholm, Sweden, on the isolation and structure determination of heartwood constituents, and with Professor Gilbert Stork at Columbia University on natural product total synthesis.
Dr. Topliss joined the Schering Corporation (now Schering-Plough) as a synthetic medicinal chemist in 1957, and in the following years worked primarily in the diuretic, antihypertensive, CNS, and antiandrogen areas. In a roughly 10 year period he and his research group synthesized and patented 5 drugs (trichlormethiazide, diazoxide, halazepam, quazepam, and flutamide) which were subsequently marketed.
Seeking a more rational, theoretically based approach to analog synthesis than was generally employed at that time, Dr. Topliss was one of the early medicinal chemists in the pharmaceutical industry to use quantitative structure-activity relationships (QSAR) methodology. This led him to formulate Operational Schemes for Analog Synthesis in Drug Design (later known as the Topliss Tree) published in 1972, and also a related Manual Hansch Approach published in 1977, which are simplified non-mathematical approaches for rapidly optimizing benzene ring substitution for potency enhancement in a compound series based on physicochemical principles. The methodology was widely adopted by medicinal chemists and is still in current use. It has been extensively cited in the literature and described in many textbooks on medicinal chemistry and specialized textbooks on drug design.
Another very significant contribution of Dr. Topliss was his identification of the dangers of being misled by chance correlations in quantitative structure-activity relationships which can occur when too many variables are screened in relation to the number of observations. He published a preliminary study on this phenomenon in 1972 and was the first to delineate the problem. This was important because the use of this type of analysis was in an exponential growth phase at the time. It was followed by a more detailed and definitive study published in 1979 which has become a standard reference on this subject.
He also edited a book “Quantitative Structure-Activity Relationships of Drugs” published in 1983, which provided a comprehensive, critical account of applications of QSAR methodology across different therapeutic areas in terms of their contributions to medicinal chemistry.
As his career advanced Dr. Topliss became progressively more involved with management responsibilities at Schering-Plough and in 1975 he was appointed to the position of Senior Director of Chemical Research. In 1979 Dr. Topliss took a new position at Warner-Lambert/Parke-Davis as Director of Chemistry and over the next 12 years he oversaw a large expansion of chemistry operations. He was promoted to Vice President, Chemistry in 1983. In 1990, recognizing the potential of combinatorial chemistry applied to the synthesis of drug-like non-peptide compounds at a time when it was only used for peptides, he established a group specifically devoted to this mission and Warner-Lambert/Parke-Davis became the first pharmaceutical company to develop and utilize such a capability (Diversomer® technology). During the time of his leadership of Chemistry two highly successful drugs, quinapril (Accupril®) and atorvastatin (Lipitor®) were invented and synthesized by chemists in the department.
In 1992 Dr. Topliss became Professor of Medicinal Chemistry in the College of Pharmacy at The University of Michigan, having served there as Adjunct Professor since 1983. Here he carried out research on the prediction of drug bioavailability resulting in the first formulation of a QSAR model for drug human bioavailability, published in 2000, enabling in-silico predictions of oral bioavailability in humans for unsynthesized compounds to be made.
In the medicinal chemistry community Dr. Topliss has served on many committees and organized various symposia sessions. He was Program Chairman for the 1974 ACS Medicinal Chemistry Symposium at The University of New Hampshire, Chairman of the Gordon Conference on Quantitative Structure-Activity Relationships in Biology in 1979, and Chairman of the Medicinal Chemistry Gordon Conference in 1985. He was active over many years in the Medicinal Chemistry Section of IUPAC, serving as President from 1992-1995 and Past-President from 1996-1999.
Over his career in medicinal chemistry Dr. Topliss has authored or co-authored some 62 papers, reviews, books and book chapters and given 70 invited talks at scientific meetings, academic institutions and companies throughout the world. He is also inventor on 33 patents.
In 1986 Dr. Topliss was elected a Fellow of the American Association for the Advancement of Science and in 1998 he was the recipient of the ACS Division of Medicinal Chemistry Award.
Monroe E. Wall, Ph.D. served as Chief Scientist in Chemistry and Life Sciences at the Research Triangle Institute. Dr. Wall studied at Rutgers University, New Brunswick, NJ, where he received B.S. (1936) and M.S. (1938) degrees in chemistry and a Ph.D. degree in agricultural biochemistry (1939). In 1941, Dr. Wall joined the Department of Agriculture's Eastern Regional Research Laboratory. He directed a research group in the first large-scale screening of plant products for potential precursors of cortisone and other steroids. More than 7,000 plants were collected, and the group's findings led to the preparation of cortisone. In 1958, his group discovered that extract of Camptotheca acuminata had antitumor activity. Dr. Wall came to RTI in 1960 from the USDA specifically to start a chemistry research group. In addition to carrying on his own research, he served as research vice president from 1971 to 1983, during which time he helped build RTI’s staff and capabilities in the areas of analytical and environmental chemistry, life sciences and bioorganic chemistry, organic and medicinal chemistry, and toxicology.
In addition to the Kettering Prize, the highest honor in the field of cancer research, Dr. Wall was the recipient of the USDA Superior Accomplishment Award, the American Pharmaceutical Association’s top research prize for natural products chemistry, and the Research Achievement Award of the American Society of Pharmacognosy. In 1998 he was awarded the American Chemical Society’s Alfred Burger Award, the most prestigious award in medicinal chemistry. The Wall-Wani discoveries of Taxol and camptothecin in the 1960s helped revolutionize modern cancer research. Dr. Wall worked at RTI until he died in 2002 at the age of 85.
Simon Campbell is a synthetic organic chemist who received his BSc (1962) and PhD (1965) degrees from Birmingham University in the UK. He carried out postdoctoral research in Birmingham and Chile, then at Stanford University with W.S.Johnson, before being appointed Visiting Professor at the Universidade de Sao Paulo, Brasil in 1970.
In 1972, Sir Simon joined Pfizer Central Research, Sandwich, as a medicinal chemist, and he retired in October 1998 as Senior Vice President for World-wide Discovery and Medicinals R&D Europe. He has co-authored over 120 publications and patents, and was a key member of the research teams that discovered doxazosin (CarduraTM) and amlodipine (NorvascTM). Both of these novel medicines became the leading agents worldwide in their therapeutic class. In addition, he was senior author on the research proposal that led to sildenafil (ViagraTM), the first oral treatment for male erectile dysfunction.
Sir Simon’s scientific contributions have been recognised by the Royal Society of Chemistry Award for Medicinal Chemistry (1989), the Herschberg Award from the American Chemical Society (1997), ACS Medicinal Chemistry Hall of Fame (1997), the Industry Research Institute (US) Achievement Award (1998), the CIA Individual Achievement Award (2006), Galen Medal (2007), the Sir James Black Award for Drug Discovery (2012) and the inaugural RSC-BMCS Lifetime Achievement Award (2015). He was elected Fellow of the Royal Society (1999), Fellow of the Academy of Medical Sciences (2003) and was admitted to the degree of Doctor of Science honoris causa by the University of Kent at Canterbury (1999), the University of Birmingham (2004) and St Andrews University (2008). Sir Simon served as President of the Royal Society of Chemistry (2004-06), and was awarded a CBE in the Queen’s 80th Birthday Honours List (2006) “for services to science” followed by a knighthood in 2015 “for services to chemistry”. He was named number 31 in the Times Eureka list of 100 top UK scientists for 2010, and was also included in the Science Council 100 Leading Practising Scientists 2014.
Sir Simon has served on various professional and research bodies including SERC Organic Chemistry Sub-Committee, Science Board, LINK Asymmetric Synthesis, ABPI R&D Committee, Chemistry RAE Panel (2001) and as Visiting Professor at the University of Leeds and Birkbeck College. He also acted as the first Chair of the Expert Scientific Advisory Committee for MMV (Geneva, 1999-2003) which he re-joined in 2008 and 2017, and was a member of the BP Technology Advisory Council (2000-04), the Council of the University of Kent (1999-2007), Advisory Council for the Misuse of Drugs (2007-09) and the Council of the Royal Society (2011-2013).
Currently, Sir Simon acts as an independent scientific consultant for Pharma, Biotech, charities, funding agencies and venture capital, nationally and internationally. He also co-chairs the Royal Society Science, Industry and Translation Committee. Sir Simon is a Fellow of the Royal Society of Chemistry, and a member of the American Chemical Society and the Society for Medicines Research
Professor of Medicinal Chemistry & Professor Emeritus of Medicinal Chemistry of the faculty of the College of Pharmacy of the University of Iowa
Joseph G. Cannon received the B. S. degree in Pharmacy (High Honors) from the University of Illinois in 1951. He subsequently received the M. S. (1953) and Ph.D. degree in Chemistry (Pharmacology minor) from Illinois in 1957.
He was appointed an Assistant Professor in the School of Pharmacy of the University of Wisconsin in 1956 and he was named Associate Professor in 1960. He joined the faculty of the College of Pharmacy of the University of Iowa in 1962 and he was named Professor of Medicinal Chemistry at that institution in 1965. He was granted the title of Professor Emeritus of Medicinal Chemistry in 1996.
His early research addressed the conformational chemistry of depolarizing myoneural blocking agents related to succinyl dicholine and the three-dimensional geometry of acetylcholine. A compound resulting from this latter study was trans-ACTM, in which the elements of the flexible acetylcholine molecule were incorporated into a rigid cyclopropane ring system, freezing the acetylcholine portion in an extended conformation. This compound is a muscarinic agonist displaying equi-potency and activity to acetylcholine itself and lacking effect at nicotinic receptors. trans-ACTM is perhaps the only known synthetic acetylcholine congener which is as good a substrate for acetylcholinesterase as is acetylcholine.
Cannon and his pharmacologist collaborator J. P. Long investigated the chemistry, structure-activity relationships, and pharmacology of apomorphine and of many of its analogs and congeners. This work led to an extended search for anti-Parkinsonian agents involving, inter alia, conformational studies on dopamine and the design, synthesis, and structure-activity studies of many analogs and congeners. An offshoot of the work on dopaminergic agonists was the unexpected discovery of new compounds having specific effects at serotonin 5-HT1A receptors. The Cannon-Long groups conducted extensive synthetic, structure-activity, and pharmacological studies on hemicholinium (a blocker of choline uptake into cholinergic nerve terminals) as a part of an overall search for prophylactic agents against phosphorus-containing “nerve gases” and insecticides. Compounds were designed which were prophylactic against fivefold LD50 doses of the phosphorus-derived insecticide paraoxon.
In 1984 he was named Dale E. Wurster Research Fellow in the College of Pharmacy and he received the Iowa Regents Award for Faculty Excellence in 1994. In 1997 he was named recipient of the Smissman Bristol Myers Squibb Award in Medicinal Chemistry
He originated and taught an American Chemical Society short course, “Pharmacology for Chemists” which he presented many times over some 27 years. In 2006 he received an ACS Outstanding Teacher Award, incident to his work with this short course He participated in the founding of the Residential School on Medicinal Chemistry presented annually at Drew University, and for many years he taught in the School.
He served on the editorial boards of the Journal of Medicinal Chemistry, Chirality, Annual Reports in Medicinal Chemistry, the Indian Journal of Heterocyclic Chemistry, and the Sixth Edition of Burger’s Medicinal Chemistry and Drug Discovery. He served as the Book Review Editor of theJournal of Medicinal Chemistry until his death in December of 2011.
Chief of the Chemical Biology Research Branch of the National Institute on Drug Abuse at the National Institutes of Health
Dr. Kenner Rice is Chief of the Chemical Biology Research Branch of the National Institute on Drug Abuse at the National Institutes of Health. His research over the past thirty-five years at the NIH has focused on the elucidation of the structure and function of neurotransmitter systems in the mammalian central nervous system (CNS) in normal, drug-altered and pathological states and the molecular mechanism of action of CNS active drugs. He has applied organic medicinal chemistry to study the mechanism of action of abused drugs and the development of medications for the treatment and prevention of drug abuse. This work has provided potential medications, many new research tools and valuable technology for drug abuse research.
One of Dr. Rice's major contributions is his development of the NIH Opiate Total Synthesis, which allows synthetic production of medical opiates and their antagonists in any desired quantity thus offering independence from foreign sources of opium, obviates concerns about potential future opium shortages (as occurred in 1973-1975), and offers opium poppy eradication as a worldwide strategy for the elimination of illicit heroin production. This synthetic route also provides the unnatural mirror image opiate isomers as invaluable research tools and potential new nonnarcotic drugs. Other highly significant contributions emanating from his program include: (a) the discovery of an imaging agent for positron emission tomography that has proven useful for study of the opioid receptor-endorphin system in conscious humans, and (b) the recent development of medications that prevent cocaine self-administration in rhesus monkeys without affecting control behavior. A single dose of one of these agents virtually eliminated cocaine self-administration for nearly 30 days. These agents may be useful as medications for the treatment and prevention of human cocaine and methamphetamine abuse for which there are no effective therapies.
Dr. Rice received his BS degree from the Virginia Military Institute in 1961. He then received his doctorate in organic chemistry from the Georgia Institute of Technology in 1966, where he also conducted postdoctoral work. He conducted antimalarial research at Walter Reed as an active duty member of the Army, and also was a Senior Scientist at Ciba-Geigy for three years, before joining the NIH in 1972. During this time, he has trained 73 postdoctoral fellows, many of whom have now gone on to prominent scientific positions in industry, government, and academia. He has received 11 previous major awards, including the ACS Division of Medicinal Chemistry Award in 1996. In 2007, he received the prestigious Smissman Award, sponsored by Bristol-Myers Squibb.
Dr. Anderson received a B. S. in chemistry from the University of Vermont in 1959 and a Ph.D. in chemistry from the University of New Hampshire in 1963. After postdoctoral work at Cornell University, he joined Merck Sharp and Dohme Research Laboratories where he rose through the ranks to become Vice President for Chemistry at West Point. In 1994 he retired from Merck to become the Senior Vice President for Chemical and Physical Sciences at the Dupont-Merck Pharmaceuticals Company that became Dupont Pharmaceuticals Company in 1998. In 1997 Dr. Anderson served as President of the American Chemical Society.
He received the E. B. Herschberg Award for important discoveries in medicinally-active substances from the American Chemical Society in 1995. He received a Doctor of Science Honoris Causa from the University of Vermont (1998) and a Doctor of Chemistry Honoris Causa from the University of New Hampshire (2001). Dr. Anderson was the recipient of the American Chemical Society Award in Industrial Chemistry in 2001, the Perkin Medal in 2002 and the National Academy of Sciences Award for Chemistry in Service to Society in 2003. In 2006 the American Chemical Society recognized Dr Anderson with its highest honor, the Priestley Medal.
Howard J. Schaeffer Chair in Pharmaceutical Sciences, College of Pharmacy, The University of Arizona, Tucson
LAURENCE H. HURLEY, Howard J. Schaeffer Chair in Pharmaceutical Sciences, College of Pharmacy, The University of Arizona, Tucson, was born in 1944 in Birmingham, England. He received his B.Pharm. (Honors) in 1967 from Bath University and his Ph.D. (Medicinal Chemistry) in 1970 from Purdue University.
Dr. Hurley’s present research interests are in the areas of design and development of antitumor agents. Over the last twenty years, work from his laboratory has led to elucidation of the structures of the drug–receptor complexes for seven different groups of compounds that are potentially useful in the treatment of cancer. In cooperation with the pharmaceutical industry, several drugs developed with the aid of these studies have been evaluated in phase I and II clinical trials. Most recently, his research has centered on secondary DNA structures, particularly G-quadruplexes as gene targets for drug design. A first-in-class G-quadruplex-interactive compound developed from technology and a lead compound licensed from The University of Arizona and The University of Texas was advanced into phase II clinical trials by Cylene Pharmaceuticals in 2007.
Dr. Hurley has been a consultant to a number of pharmaceutical companies and is currently a Senior Editor for Journal of Medicinal Chemistry. He is now also a member of the NCI Scientific Board of Councilors. He is a recipient of the 1988 George Hitchings Award in Innovative Methods in Drug Design, the 1989 Volwiler Research Achievement Award from the American Association of College of Pharmacy. He is the recipient of the 1992 APhA Research Achievement Award in Medicinal Chemistry and the 1994 American Chemical Society Medicinal Chemistry Award. In 2005 he was awarded the George & Christine Sosnovsky Award in Cancer Therapy by the Royal Society of Chemistry, and in 2007 he was inducted into the American Chemical Society Medicinal Chemistry Hall of Fame. He is also the recipient of a number of lectureships, including the 2001 Frank Rose Memorial Lecture at the British Association for Cancer Research. In 1996 he was awarded a D.Sc. degree from Bath University.
Dr. Arthur A. Patchett was born on May 28, 1929 in Middletown, New York. He is a summa cum laude graduate of Princeton in 1951 where he majored in chemistry. He was a Fulbright Scholar at Cambridge University (1951 – 1952) and his Ph.D. in chemistry was awarded from Harvard in 1955. His thesis research on the synthesis of lanostenol was done under the direction of Prof. R. B. Woodward.
During 1955 – 1957 Patchett did post-doctoral research with Dr. Bernhard Witkop at the National Institutes of Health. The syntheses of amino acid analogs and some biochemical mechanism studies were done during this period. In 1957 he joined the Merck Research Laboratories working first on analgesics, steroids and antibacterial agents. He became a director of the Synthetic Chemistry Department in 1962 and groups under his personal direction synthesized the anti-inflammatory drug Diflunisal®, androgen biosynthesis inhibitors and topically active steroidal anti-inflammatory agents.
In 1972 Dr. Patchett became director of the New Lead Discovery department. Compounds for biological screening were prepared by synthesis and from natural product sources. A fermentation products for screening project supplied extracts of fungi and Streptomyces whose activity in other programs suggested they might be producing metabolites worthy of broader testing. An important and influential discovery of this project was the HMG-CoA reductase inhibitor Mevacor which became the first statin drug to be marketed for cholesterol lowering. Another Merck group added a methyl group to Mevacor® to improve the metabolic stability of its ester side chain. The resultant more active product Zocor® became a major product for Merck. Other research groups have produced the statin drugs Pravachol, Lipitor® and Crestor® in all cases retaining the active site functionality of Mevacor®.
The synthesis of enzyme inhibitors was another strategy of the New Lead Discovery Department. α-Fluoromethyl amino acids were designed as potent, irreversible decarboxylase inhibitors which could effectively and specifically inhibit the formation of histamine and noradrenaline. Phosphinic acids were mechanism activated, virtually irreversible inhibitors of a bacterial target D-Ala-D-Ala ligase. Most significant were the syntheses of the orally active, non-sulphydryl angiotensin converting enzyme (ACE) inhibitors Vasotec® and Prinivil®. They had a longer duration of action and less side effects than the innovative -SH containing ACE inhibitor Capoten®. Vasotec® and Prinivil® became widely used therapy in the treatment of hypertension and congestive heart failure.
A second consequential accomplishment of the fermentation products screening project was the discovery of the cholecystokinin antagonist asperlicin. Another Merck group increased its potency by designing much simpler analogs of its benzodiazepine core. The latter they called a privileged structure and they recommended that such recurring ligands in G-protein coupled receptors are a good starting point in the design of agonists and antagonists. Dr. Patchett’s group developed this idea with the synthesis of libraries of dipeptides linked to privileged structures. One of them became the lead for a potent, clinically active growth hormone secretagogue MK-0677. The same strategy led to dipeptidyl privileged structure derivatives which are potent and selective somatostatin and melanocortin MC4 agonists. Thus the dipeptidyl privileged structure design were shown to have some generality in generating agonists of much larger peptides whose message is contained within a reverse turn sequence.
In 2002 Dr. Patchett joined the NeoGenesis scientific advisory board and when they were acquired by Schering-Plough in 2005, he became one of their consultants, a position which he currently holds.
Dr. Patchett is the co-author of 182 papers and 183 issued US patents. He was chairman of the ACS Division of Medicinal Chemistry (1971), was co-chairman of the Drew University Residential Course in Medicinal Chemistry (1987-2000), and was a member of the Chemistry Department Advisory Council of Princeton University (1996-2000). He was a member of the editorial board of Medicinal Research Reviews (1991-1998). Dr. Patchett was inducted into the New Jersey Inventors Hall of Fame (1990), became a fellow of the AAAS (1994) and he received a Doctorate of Science (hon.) from Bloomfield College (2001). Merck funded in his honor the Arthur Allan Patchett Professorship at Princeton (2001).
Dr. Patchett’s awards include the Merck Directors’ Scientific Award (1987 and 1989), the Pharmaceutical Manufacturers Association Discoverers’ Award (1992), the American Chemical Society’s E. B. Hershberg Award (1993), the Smissman Bristol-Myers Squibb Award (2001), the American Chemical Society’s Alfred Burger Award in Medicinal Chemistry (2002) and the National Academy of Sciences Award for Chemistry in Service to Society (2007).
Professor Leroy B. Townsend’s scholarship has earned him worldwide recognition and a reputation for excellence in the design and synthesis of heterocyclic compounds and nucleosides as potential agents to treat cancer and infectious diseases. Cancer research is the area in which Leroy first was recognized for major contributions. He and his collaborators were the first to accomplish a total synthesis of the naturally-occurring nucleoside antibiotics tubercidin, toyocamycin and sangivamycin. The latter compound was advanced to clinical testing. He and his group also were the first to synthesize more than ten other nucleoside antibiotics including the first in a new class of compounds, C-nucleoside antibiotics. This work included not only synthetic chemistry but also the development of new physical-chemical techniques for elucidation and proof of structure. Other work in the nucleoside area led to the synthesis of triciribine, a compound which has advanced to phase II clinical investigations for ovarian cancer.
Leroy also has been successful in research aimed at developing drugs to treat parasitic diseases. His studies sponsored by the World Health Organization (W.H.O.) led to the design and synthesis of a series of benzimidazole heterocycles which are active against filariasis – a disabling parasitic disease prevalent in tropical climates. The compounds which Leroy has discovered are very active in low dosage and are the only compounds known which are active against both the juvenile and adult forms of the worm. Preclinical pharmacology and toxicology studies are now advancing toward a trial of the most promising of these compounds in humans. The Director of Tropical Diseases for W.H.O., Dr. Tore Godal, has commended Leroy for his pioneering work in this area and has made the development of these compounds a high priority.
Recent significant progress has been made in Leroy's work with antiviral drugs. In collaboration with Professor John Drach, two series of compounds have been discovered which are highly active against human cytomegalovirus (HCMV) – the virus which causes retinitis in AIDS patients, pneumonitis in bone marrow transplant patients, and is one of the leading causes of birth defects in the U.S. These new compounds are active against HCMV at non-toxic concentrations and are active against drug-resistant strains of the virus because they act by a new mechanism. In collaboration with colleagues at Glaxo Wellcome Co., an analog of these compounds has been made which has undergone successful preclinical evaluation and now is completing successful phase II clinical trials. In addition to these compounds, another compound (triciribine, mentioned above) recently has been found to be active against HIV and to act by a new mechanism. For a single individual to discover drugs which may be used to treat a diversity of diseases such as cancer, filariasis, herpes, and AIDS is extremely significant and highly unusual. These discoveries are a result of hard work and a broad diversity of talents; namely, Leroy's ability to lead and inspire students and collaborators plus his considerable knowledge in both chemistry and relevant biology.
During this time of great productivity in research and scholarship, Leroy also has been very active in service to local, national, and international scientific groups and organizations. He was co-founder of the International Roundtable on the Chemistry and Biological Activity of Nucleosides & Nucleotides, and co-founder of the International Society of Heterocyclic Chemistry. He has served as president of the International Society of Heterocyclic Chemistry and has held virtually every elected position, including chairman, of the 8000-member Division of Medicinal Chemistry of the American Chemical Society. He also has served on grant review bodies and study sections for the National Science Foundation, the American Cancer Society, the National Institutes of Health (in both bioorganic chemistry and in medicinal chemistry), the Canadian Heritage Foundation, NATO, the World Health Organization, the World Health Organization steering committee on the chemotherapy of malaria, and the advisory committee on AIDS to the director of the National Institute of Allergy and Infectious Diseases. Locally, he has headed the Drug Discovery Group of the Comprehensive Cancer Center, is a member of that center's operating committee, has served as the College of Pharmacy's representative to the Medical Research Council, has been a member of the College's Executive Committee, and served on numerous search committees. He is a member of the editorial board of several significant journals in heterocyclic and nucleoside chemistry, as well as the editor and author of a very important series of books on organic synthesis entitled, "Improved and New Synthetic Procedures, Methods, and Techniques." This series now contains six volumes with more in preparation. Recently, he has been selected to serve on the editorial board of Burger’s Medicinal Chemistry, 6th Edition. Leroy also has been the organizer of local and national meetings as well as international symposia. His most recent effort was organizing and chairing the very successful 25th National Medicinal Chemistry Symposium which was held at the University of Michigan in 1996. His selection as chair was unique because he became the only Division member to chair two National Medicinal Chemistry Symposia, the 15th at the University of Utah and the 25th at Michigan. Other awards and elected positions are too numerous to list here, but are documented in his curriculum vitae.
Professor Townsend is no less energetic in his dedication to his students and to teaching. He has taught pharmacy students, undergraduate and graduate medicinal chemistry students, and chemistry students with distinction. He has mentored research projects for undergraduate students, minority undergraduate students, high school students (summer programs), M.S. students, Ph.D. students, and postdoctoral fellows. His demanding but friendly mentoring of students has resulted in exceptional training of, and exceptional performance by, students fortunate enough to be chosen as a part of his research group. His Saturday morning research group meetings have become a virtual institution with his students and postdoctoral fellows. These regular meetings serve as an arena for training in research methodology, discussion of research results, critiques of scientific literature, and training in the preparation and review of publications and grants. This is teaching which goes well beyond that of the usual classroom. In addition to individual and didactic instruction, Professor Townsend has chaired the Interdepartmental Graduate Program in Medicinal Chemistry (for twenty years) and has restored it to a preeminent national program. He has also served as co-principal investigator and principal investigator of the Pharmacological Sciences Training Program. This is a unique, large training program and grant which provides students with the option of Ph.D. studies in one of several disciplines. The program trains students from seven University departments; namely medicinal chemistry, pharmacology, pharmaceutics, chemistry, biological chemistry, physiology, and toxicology.
In the last several years Leroy’s accomplishments have been recognized by a number of institutions and organizations. Specifically, in 1993 he received the Distinguished Faculty Award for the University of Michigan from the Michigan Association of Governing Boards of State Universities. In 1994 he received the Division of Medicinal Chemistry’s Edward E. Smissman - Bristol Myers Squibb Award. In 1994 he also received the T.O. Soine Memorial Lecturer Award from the University of Minnesota and the Distinguished Alumnus Award from New Mexico Highlands University. In 1995 he became a Fellow of the American Association for the Advancement of Science. In 1996 he again was elected as an academic councilor for the Division of Medicinal Chemistry of the American Chemical Society. In 1997 he received an honorary Doctor of Science degree from the University of Nebraska. In 1998 he was honored for co-founding the International Roundtable on the Chemistry and Biological Activity of Nucleosides & Nucleotides. This year (1999) he was the recipient of an honorary doctorate (honaris causa) of the University from the Universite Montpellier II, France. He was recently nominated to stand for election as the chairman of the Pharmaceutical Sciences Division of the American Association for the Advancement of Science. He was also nominated to stand for election as a director of the International Society of Antiviral Research.
Dr. Daniel H. Rich, Emeritus Ralph F. Hirschmann Professor of Medicinal And Organic Chemistry at the University of Wisconsin-Madison, was born December 12, 1942 in Fairmont, Minnesota. He was a General Motors Scholar at the University of Minnesota-Minneapolis from 1960-64 and received the B. Chemistry degree in 1964 (working with Wayland E. Noland). He received his Ph. D. in organic chemistry from Cornell University in 1968 (with A. T. Blomquist). He held postdoctoral appointments with Nobel Laureate Vincent du Vigneaud (Cornell University) and W. S. Johnson (Stanford) before joining the Faculty in Pharmacy at the University of Wisconsin-Madison in 1970. Dr. Rich was Professor of Medicinal Chemistry in the School of Pharmacy and Professor of Chemistry in the Department of Chemistry at UW-Madison. His research focused on the synthesis and conformational analysis of cyclic peptides, and the design and synthesis of inhibitors of therapeutically important enzymes, especially aspartic proteases. His work in the aspartic protease field laid the ground-work for the development of the HIV protease inhibitors used to treat AIDS. He has published over 250 articles and trained 36 PhD students and another 100 postdoctoral students; many of his students rose to important research positions in the pharmaceutical industry.
His research accomplishments have been recognized by the 1990 Vincent du Vigneaud Award in Peptide Chemistry, the 1992 ACS Division of Medicinal Chemistry Award, the 1992 Research Achievement Award of the American Association of Pharmaceutical Scientists, the 1992 George Herbert Hitchings Award for Innovative Methods in the Design and Discovery of Drugs, the 1993 ACS Ralph F. Hirschmann Award in Peptide Chemistry, a WARF University Professorship at UW-Madison in 1994 (which he named after Ralph F. Hirschmann), the E. Volwiler Research Achievement Award from the Amer. Assoc. Colleges Pharmacy in 1995, an Arthur C. Cope Scholar Award from the American Chemical Society in 1999 and the R. Bruce Merrifield Award from the American Peptide Society in 1999, and the E. E. Smissman Award from the ACS Division of Medicinal Chemistry in 2005. In 1993, he was a Senior U.S. Scientist Alexander von Humboldt Scholar in Germany. In 2004, he was awarded an Outstanding Alumni Achievement Award from his alma mater, the Institute of Technology of the University of Minnesota.
Professor Rich was elected Teacher of the Year by the UW-Madison Pharmacy graduating class of 1986 for his teaching of Medicinal Chemistry. From 1989 till his retirement in 2006 he lectured each year at the Drew University Residence School in Medicinal Chemistry on the design of enzyme inhibitors and peptidomimetics. In addition, Professor Rich has presented short courses in Medicinal Chemistry to pharmaceutical societies in Sweden, England, Japan and other foreign countries. He presented about 20 invited lectures each year, nationally and internationally. Professor Rich also served as a consultant in drug-design and discovery, especially in the area of design of protease inhibitors, for many major pharmaceutical companies.
Professor Rich served in administrative roles at UW-Madison. From 1976-1980 he was Assistant Dean of Graduate Studies in the School of Pharmacy. He served as elected member of the Physical Sciences Divisional Committee for UW-Madison from 1991-1993 and chaired the committee in 1992-1993. He was appointed to the UW-Madison Graduate School Research Committee (Biology Division) from 1994 to 1997. He also served as a member of the honorary degrees committee for UW-Madison from 1995-1998. He organized and wrote the first Chemistry-Biology Interface training grant for UW-Madison in 1992 and served as its program director, principle investigator and chair of the advisory committee from 1993-2003; the UW-Madison CBI training program remains the largest of its type in the United States. From 2005-2006, he was Associate Dean for Research and Graduate Studies for the School of Pharmacy.
At the national level, Professor Rich was President of the American Peptide Symposium from 1979-1981, a member of the Bioorganic and Natural Products study section for NIH from 1981-1985 and Chairman of that study section from 1983-1985, a Fellow of the American Association for the Advancement of Science since 1986, and a council member for the American Peptide Society. He was Associate Editor for the Journal of Medicinal Chemistry from 1988-1992, and was Associate Editor of the ACS journal, Organic Letters, from 1999 through 2005.
Professor Rich was active within the Medicinal Chemistry Division of the American Chemical Society. He was Chairman for the Division of Medicinal Chemistry in 1992, served as a member of the Planning Committee, organized two Symposia for the Division, and was an Academic Councilor for the division. He organized the 29th National Medicinal Chemistry Symposium held June 27-July 2, 2004 in Madison WI.
George deStevens was born in Tarrytown, New York. He earned his B.S., M.S., and Ph.D. in organic chemistry and enzymology at Fordham University. In 1955 he joined Ciba Pharmaceutical Company, where he discovered the diuretic hydrochlorothiazide. He left Ciba-Geigy in 1979 to join the faculty of Drew University.
In 1991, Dr. deStevens was the first recipient of the E.B. Hershberg Award of the ACS.
Arnold Brossi was born in Switzerland in 1923. He earned his Ph.D. at the ETH in Zurich in 1952 and subsequently joined Hoffman-La Roche. He joined the National Institutes of Health in 1976, where he led the Medicinal Chemistry Section of the National Institute of Diabetes and Digestive and Kidney Diseases. He retired in 1991. He became Research Professor in the School of Pharmacy at the University of North Carolina.
Dr. Brossi authored over 400 scientific papers and held many patents. He was a member of the Advisory Board of Organic Synthesis. Dr. Brossi was the 1990 winner of the GlaxoSmithKline Alfred Burger Award of the ACS.
Distinguished Professor in the Department of Medicinal Chemistry of the faculty of the College of Pharmacy at the University of Minnesota
Professor Portoghese received his Ph.D (1961) in medicinal chemistry from the University of Wisconsin, Madison. He then joined the faculty of the College of Pharmacy at the University of Minnesota where he presently is Distinguished Professor in the Department of Medicinal Chemistry.
Over the years Professor Portoghese has maintained an active research program and has trained approximately 100 graduate students and postdoctorals. He has published over 350 scientific papers and he is listed in the ISI database of Highly Cited Researchers. He has received numerous awards from national and international scientific societies, the most recent being the Nauta Award (2006) given by the European Federation of Medicinal Chemistry. The American Chemical Society’s awards include the prestigious Alfred Burger Award (2000), the Medicinal Chemistry Award (1990), and the Smissman Bristol-Myers Squibb Award (1991). Other awards include the Ernest H. Volwiler Award (1984), which is the highest research recognition presented by the American Association of Colleges of Pharmacy; and two Research Achievement Awards in Medicinal Chemistry given by the American Association of Pharmaceutical Scientists (1990) and the Academy of Pharmaceutical Scientists of the American Pharmaceutical Association (1980). The fact that he is recipient of the Eddy Award (1991, College on Problems of Drug Dependence) and Founders Award (2000, International Narcotics Research Conference) whose members are primarily biologists, illustrates that his scientific contributions are also recognized outside the discipline of medicinal chemistry. His achievements have been recognized by the University of Minnesota, and include his induction into the Academy of Excellence in Health Research (2003); Citation of Excellence in Teaching, Research, and Service (2000); and the Weaver Medal (2001). He is recipient of a Citation (1996) from the University of Wisconsin (Madison) and he has been recognized abroad with honorary doctorate degrees from the University of Catania (1986) and the Royal Danish School of Pharmacy (1992). The importance of his research has been recognized by the National Institutes of Health with a MERIT Award (1997).
His broadest impact on medicinal chemistry has been as Editor-in-Chief of the Journal of Medicinal Chemistry (JMC). Over the past 35 years he has shaped the Journal into the world’s most prestigious and most highly cited (impact factor, 5.1) medicinal chemistry journal. The Journal presently has nine editors in the U.S. and Europe. Altogether, the Journal accounts for more than 25% of all citations in the field.
University Distinguished Professor in the Department of Medicinal Chemistry at the University of Kansas
Dr. Lester A. Mitscher, University Distinguished Professor in the Department of Medicinal Chemistry at the University of Kansas, received his Ph. D. degree in Chemistry in 1958 from Wayne State University, Detroit, where he worked on the structure of coffee oil diterpenes and on optical rotatory dispersion under Carl Djerassi. He continued his work on natural product chemistry at Lederle Laboratories from 1958-1967 where he rose to group leader in antibiotic discovery until he accepted an assistant professorship in Natural Products Chemistry at The Ohio State University (1967), rising soon to the position of Professor. In 1975 He accepted a University Distinguished Professorship and Chairmanship in the Department of Medicinal Chemistry at Kansas University. He returned to the faculty in 1992 where he remains. He has conjoint academic appointments at the University of Missouri-Kansas City and the Victorian College of Pharmacy, Melbourne, Australia. His academic studies have centered about spectroscopy, synthesis, screening and structure determination primarily of naturally occurring antimicrobial, anticancer and antimutagenic agents, and development of combinatorial methodologies. He has published actively in the field of herbal medicines. Overall he has published more than 270 research publications and authored or coauthored seven technical books on drug discovery and properties and is on the editorial board of several technical journals. He is a member of the executive committee of the International Organization for Chemistry in Developing Countries and has traveled extensively internationally lecturing and performing research. He consults extensively in the Pharmaceutical Industry and for the National Institutes of Health. His research awards include the Smissman Award in Medicinal Chemistry (American Chemical Society), Volweiler Award (American Association for Pharmaceutical Education), the Research Achievement Award in Natural Products Chemistry (American Pharmaceutical Association), the Award in Medicinal Chemistry (Medicinal Chemistry Division, American Chemical Society), The Norman Farnsworth Research Achievement Award (American Society for Pharmacognosy) and is an Elected Fellow American Association for the Advancement of Science and a member of the Medicinal Chemistry Roll of Honor of the American Chemical Society.
Professor of Biochemistry and Molecular Biophysics & of Biomedical Engineering at Washington University in St. Louis
Garland R. Marshall is Professor of Biochemistry and Molecular Biophysics and of Biomedical Engineering at Washington University in St. Louis. In 1979, he founded Tripos Associates (NASDAQ:TRPS), vendor of computer-aided molecular design software, and was its President and Chairman until 1987. Dr. Marshall received the 1988 Award in Medicinal Chemistry and the 1996 Midwest Award in Chemistry from the ACS. He was recently selected for the ACS Medicinal Chemistry Hall of Fame. Awards in peptide chemistry include the 1994 Vincent du Vigneaud Award, the 2000 Cathay Award (Chinese Peptide Society) and the prestigious 2001 Merrifield Award (American Peptide Society). Prof. Marshall founded MetaPhore Pharmaceuticals Inc. in 1995. Prof. Marshall received an Doctora Honoris Causa, Politechniki Lodzkiej, in 1993 (Technical University, Lodz, Poland). In 2005 Prof. Marshall was the Inaugural Lee Wing Nam Visiting Professor, School of Biological Sciences, Nanyang Technological University, Singapore. In 2006 he was the Smissman Lecturer at the University of Kansas, and in 2007, the Alfred Burger Lecturer at the University of Virginia. Prof. Marshall has served on the SAB of the Institute for Molecular Biosciences, University of Queensland, Brisbane, Australia, the SAB of the Drug Discovery Institute of the University of Minnesota as well as a Trustee for the Torrey Pines Institute for Molecular Sciences (La Jolla, CA and Port St. Lucie, FL). Prof. Marshall was also the founder of Metaphore Pharmaceuticals that took a drug-like superoxide dismutatase mimetic through Phase II clinical studies. He was appointed an adjunct Professor of Chemistry at Washington University in 2010, and served in the fall of 20121 as visiting Professor at the Faculta di Farmacia, Sapienza Universitá di Roma.
Prof. Marshall was the first graduate student of R. Bruce Merrifield, Nobel Laureate, and participated in the invention/development of solid-phase peptide synthesis. Much of his early research dealt with the use of constrained amino acids/dipeptides in peptidiomimetics and enzyme inhibitors. More recently, he has experimentally determined by DEER EPR the rhodopsin-bound conformation of a segment of the C-terminus of Galpha. Currently, his research focuses on development of isoform-specific inhibitors of histone deacetylaces in HIV latency, uveal melanomas and antimalarials.
Roland K. Robins earned his bachelor's and master's degrees in chemistry from Brigham Young University, followed by his Ph.D. from Oregon State University. He taught at New Mexico Highlands University, Arizona State University, and the University of Utah before joining the faculty at Brigham Young University. There he founded the BYU Cancer Research Center. His research centered on nucleoside chemistry, including compounds such as 2-chlorodeoxyadenosine (cladribine).
Dr. Robins was the 1988 winner of the GlaxoSmithKline Alfred Burger Award of the ACS.
Robert Heinz Abeles was born in Vienna, Austria on January 14, 1926. As a boy, he emigrated to the United States and settled in Chicago, Illinois. He was educated at the University of Chicago, where he received the M.S. degree in 1950. He went on to earn a Ph.D. degree in Biochemistry at the University of Colorado in 1955, and he did postdoctoral work in Chemistry with F.H. Westheimer at Harvard University. He was an Assistant Professor of Chemistry at The Ohio State University from1957 to 1960, Assistant and Associate Professor of Biological Chemistry at the University of Michigan from 1960 to 1964, and Associate Professor and Professor of Biochemistry at Brandeis University from 1964 to his death on June 18, 2000. Abeles received many honors during his career, including the Edward E. Swissman-Bristol Myers Award in Medicinal Chemistry in 1987, the Repligen Award in the Chemistry of Biological Processes in 1988, the Alfred E. Bader Award of the ACS in 1990, the William Rose Award of the ASBMB in 1994, an Alexander von Humboldt Senior Scientist Award from the German government, and an Honorary Doctor of Science degree from the University of Chicago, as well as election to the National Academy of Sciences and the American Academy of Arts and Sciences.
Professor Abeles was an imaginative and creative force in the field of mechanistic enzymology. Abeles' work relied on the confluence of chemistry and biology long before the interface of these two disciplines came into vogue. He investigated enzymatic reactions that posed mechanistic puzzles to organic chemists, and his contributions include many 'firsts'. He first discovered the mechanism of action of the vitamin B12 coenzyme adenosylcobalamin, the development of suicide inactivators for enzymes as pharmaceutical targets, the first discovery of a transition state analog inhibitor, the first discovery of the retaining double displacement mechanism in glycosyltransferases, and the first elucidation of the mechanisms of action of many enzymes that catalyze chemically novel reactions. Abeles discovered the pathway from methylthioadenosine to methionine, and he then discovered the enzymatic production of carbon monoxide, a regulator of blood-vessel relaxation.
Abeles began his career by investigating the enzymatic dehydration of 1,2-propanediol to propionaldehyde in bacteria, as a possible example of an intramolecular hydride shift. In this research he discovered and characterized dioldehydrase, which he showed to be one of the first enzymes to require a vitamin B12 coenzyme, adenosylcobalamin. The molecular basis for the action of this coenzyme was unknown. Abeles soon disproved the hypothesis of the 1,2-hydride shift and proceeded to elucidate the mechanistic role of adenosylcobalamin in hydrogen transfer. Between 1964 and 1971 every significant new finding regarding the mechanism of action of adenosylcobalamin was first discovered in Abeles' laboratory. All findings were quickly generalized in other laboratories for other adenosylcobalamin-dependent reactions. As one step in his research on dioldehydrase in the mid-1960s, Abeles discovered his first suicide inactivator, glycolaldehyde, which inactivated dioldehydrase. Abeles' work on dioldehydrase not only influenced research in biochemistry, it also introduced new chemistry, unlike any that had been described in the classical literature.
In the 1970s, Abeles turned his skills and intellect to the problem of designing and investigating specific inhibitors of enzymes. Such inhibitors are fundamental starting points in drug discovery. This work was directed toward the long-term goal of finding ways to proceed rationally to the design of pharmacological agents that might find use in the treatment of disease. Dr. Abeles was an innovative and imaginative force in this field, and his work stimulated research in the pharmaceutical industry and academia. Abeles designed potent inhibitors of proteases, carboxylases, oxidases, isomerases, and dehydrogenases. Many of these inhibitors were suicide inactivators. These compounds underwent initial steps of the normal catalytic mechanisms, leading to species that deviated from the natural course of events and led to destruction of enzymatic activity; thus, the enzyme catalysed its own death. Suicide inactivators revealed information about enzymatic mechanisms, and provided the specificity necessary for drug development.
Abeles' magnetic speaking style, originality, and creativity drew students into his orbit. He had the ability to define the essence of a research problem and then to solve it. He trained three generations of graduate and postdoctoral students to be leaders in the science of mechanistic enzymology.
Vice President/Senior Vice President of Basic Research (Rahway) at Merck, West Point (PA)
Born in Bavaria, Germany, Ralph Hirschmann came to the US in his teens. He graduated from Oberlin College before serving in the US Army for three years. He resumed his education at the University of Wisconsin (Madison) with W. S. Johnson as the Sterling Winthrop Fellow (1950). That year he was recruited by M. Tishler to join Process Research at Merck. He discovered the first rearrangement under stereoelectronic control, studied later in detail by E. J. Corey. With R. G. Denkenwalter he directed the first solution synthesis of an enzyme, announced jointly with Merrifield's solid phase synthesis in 1969.
Becoming increasingly interested in medicinal and bio-organic chemistry, he was appointed Executive Director of Medicinal Chemistry at Merck, West Point (PA) in 1974 and Vice President/Senior Vice President of Basic Research (Rahway) in 1976/1978, respectively.
Professional activities included serving on the NIH Medicinal Chemistry A Study Section, on several committees of the NSF, NRC and ACS, on over a dozen Editorial and Advisory Boards, and on the Boards of Trustees of Oberlin College, the Gordon Research Conferences, and others.
He holds three honorary Doctor of Science degrees and was elected member of the American Academy of Arts and Sciences and of the National Academy of Sciences. During his tenure as Merck's Head of Basic Research, his colleagues discovered and/or studied such blockbuster drugs as Mevacor, Vasotec, Primaxin and Ivermectin.
In 1988 he was invited to join the Department of Chemistry of the University of Pennsylvania as the first Research Professor in Chemistry. In 1994 he was appointed the Rao Makineni Professor of Bioorganic Chemistry.
Founder of BioCryst Pharmaceuticals & Executive Vice President & Chief Scientific Officer
Dr. John A. Montgomery was born in Greenville, Mississippi, in 1924. He earned his A.B. in Chemistry (cum laude) and his M.S. in organic chemistry from Vanderbilt University, and his Ph.D. in organic chemistry from the University of North Carolina.
He joined the Southern Research Institute in 1952, where he served as Director of Organic Chemistry Research (1956-1986), Vice President (1974-1981), Senior Vice President and Director of the Kettering-Meyer Laboratory (1981-1990), and was named Distinguished Scientist in 1990. He was a founder of BioCryst Pharmaceuticals and served as Executive Vice President and Chief Scientific Officer from 1990-2002. He served on the BioCryst Board of Directors until May 2004.
Dr. Montgomery invented or co-invented a number of FDA-approved anti-cancer drugs, including lomustine, carmustine, dacarbazine, fludarabine, and clofarabine.
Dr. Montgomery published over 400 scientific papers and held 51 patents. He was awarded the GlaxoSmithKline Alfred Burger Award of the ACS in 1986, and the Edward E. Smissman Bristol-Myers Squibb Award in 1995. He served on the Editorial Boards of several major journals, and held several positions in the Medicial Chemistry Division, including Chairman of the Division in 1980.
Adapted from the Dutch-language Wikipedia with the assistance and permission of Evert Ariens:
Everhardus Jacobus Ariens was a member of an important Dutch brick manufacturing family and a Dutch pharmacologist and professor at the Katholieke Universiteit Nijmegen (Radboud Universiteit Nijmegen today). He made important contributions to the understanding of the function of receptors and the mathematical description of ligand-receptor interactions (receptor theory). In addition, Ariens was the initiator for the collection of stereochemistry in drug development and has pioneered the development of enantiomerically pure drugs.
Everhardus Ariens was born on January 29, 1918 in Wijk bil Duurstede, the Netherlands, and grew up as the sixth of ten children. After a temporary stay in a boarding school, he went to the pre academic school (HBS) in Wageningen in 1935. Then he began studying chemistry at the University of Utrecht, from which he graduated in 1942, although his preference was actually biology. His studies were interrupted by the Second World War. After his refusal to sign a declaration of loyalty to the German Reich, he escaped from the territories occupied by Germany via Switzerland, France and England, and he found asylum with the U.S. Army.  He completed his unfinished study of medicine after the second world war, and received a degree in 1948 .
After the Second World War, he conducted research in the laboratory of Prof. UG Bijlsma in the area of adrenergic substances and received a double doctorate in the fields of chemistry and in medicine on the same day in 1950. In 1951, Ariens moved to Nijmegen, having been established at the local Catholic University in the Department of Pharmacology. From 1954 until his retirement, he worked as a professor.
Based on his dissertation, he developed a method for the quantification of pharmacological effects resulting from ligand-receptor interactions. To this end he introduced the concepts of affinity and intrinsic activity.  With the help of these terms he could describe the behaviour of agonists and antagonists and the dual agonist / antagonist behaviour of partial agonists. An important contribution made by Ariens was the establishment of quick and reproducible experiments on isolated organs rather than in living animals, which could quantitate the affinity and intrinsic activity of test substances.
The term antagonist was originally coined to describe different profiles of drug effects. The biochemical definition of a receptor antagonist was introduced by Ariens in the 1950s. The current accepted definition of receptor antagonist is based on the receptor occupancy model. It narrows the definition of antagonism to consider only those compounds with opposing activities at a single receptor. Agonists were thought to turn "on" a single cellular response by binding to the receptor, thus initiating a biochemical mechanism for change within a cell. Antagonists were thought to turn "off" that response by 'blocking' the receptor from the agonist. This definition also remains in use for physiological antagonists, substances that have opposing physiological actions, but act at different receptors. For example, histamine lowers arterial pressure through vasodilation at the histamine H1 receptor, while adrenaline raises arterial pressure through vasoconstriction mediated by β-adrenergic receptor activation.
E.J. Ariens was also active in the field of structure-activity relationships (SAR), a branch of medicinal chemistry. With the provocative statement that commonly used racemic drugs were 50% contaminated,  he triggered a debate among pharmacologists and medicinal chemists and alerted the drug approval agencies. Ariens work was therefore the key precursor for the targeted development of enantiomerically pure drugs. Another of his theories, surrounded his controversial view view that drug metabolism is wasteful, and he called for the development of metabolism-resistant drugs. He also continued in the tradition of Dutch pharmacologists and fought against quackery. 
Everhardus Ariens was awarded the Purkinje Medal in 1963 at the second International Congress of Pharmacology in Prague. He also received the Dr. Saal van Zwanenberg Prize (1972), the Poulsson Medal of the Norwegian Society of Pharmacology (1973), the Scheele Medal (1974), the Schmiedeberg-Medal (1980) and the Smissman Award of the American Chemical Society (1985). He was also awarded honorary doctorates by the universities Universidade Luterana do Brasil, Christian-Albrechts-University Kiel, University of Paris-Sud and Università degli Studi di Camerino. He posthumously received an honorary doctorate on March 22,2002 from the Ohio State University .
Professor Ariens was knighted by H.M. the Queen of the Netherlands to Ridder in de Orde van de Nederlandse Leeuw, and also received the following awards: Honorary citizen of the State of Texas; Member of the Royal Academy of Science of the Netherlands; Deutsche Akad. der Naturforscher Leopoldina; Acad. Royale de Médicine de Belgique; Kon. Acad. voor Geneeskunde; Kon. Acad. voor Geneeskunde. He was a corresponding member of German Pharmacological Society, an honorary member of Soc. Italiana di Scienze Farmaceutiche, Asoc. de Quimicos-Spanje, Dutch Pharmacological Society, Ac. of Pharmaceutical Sciences, South African Pharmacological Society, Kon. Ned. Chemische Ver. E.J. Professor Ariens passed away on March 3, 2002 in Nijmegen.
 H. Timmerman, DD Breimer: Everhardus Jacobus Ariens. Nederlandse Akademie van Wetenschappen Koninglijke, www.knaw.nl/publicaties/pdf/20061074_1.pdf
 P. N. Patil: Everhardus J. Ariens (1918-2002). A tribute. In: Trends in Pharmacological Sciences. Volume 23, 2002, p. 344-345.
 Ariens EJ, van Rossum JM, Simonis AM: Affinity, intrinsic activity and drug interactions. In: Pharmacol. Rev.. 9, No. 2, June 1957, p. 218-236. PMID 13,465,302th
 Ariens EJ: Stereochemistry, a basis for sophisticated nonsense in pharmacokinetics and clinical pharmacology. In: Eur J. Clin. Pharmacol .. 26, No. 6, 1984, p. 663-668. PMID 6092093
Books: E. J. Ariens: Molecular Pharmacology. Elsevier Science & Technology Books, San Diego, USA, 1967, ISBN 0120604019
In 1953, Dr. Paul Janssen started with pharmaceutical research in his parents’ company in Turnhout, Belgium. Since 1961, Janssen Pharmaceutica is part of Johnson & Johnson, the most comprehensive and broadly based manufacturer of healthcare products in the world. Janssen medicines are sold throughout the world.
Dr. Paul Janssen was one of the most productive pharmaceutical researchers of the 20th century. He and his teams discovered many break-through medicines in various disease areas, such as anesthesia and pain management, psychiatry, mycology and gastro-enterology. He has more than 100 patents on his name.
Dr. Janssen received 22 honorary doctorates worldwide, more than 80 medical awards, and was honorary member of over 30 scientific institutes and organizations.
He was author or co-author of more than 850 scientific publications and held more than 500 scientific presentations all over the world. Up until his death, Dr. Paul remained very involved in the search for new medicines for diseases afflicting humankind.
From Wikipedia, the free encyclopedia:
Hamao Umezawa (October 1, 1914 - December 25, 1986) was a Japanese scientist who discovered several antimicrobial agents and enzyme inhibitors. After graduating from the Musashi Junior and Senior High School, Umezawa completed his medical degree in 1937. After serving in the Japanese army during World War II Umezawa did work on tuberculosis which led to his discovery, in 1956, of antibiotic kanamycin. By this stage Umezawa was heading the Institute of Microbial Chemistry in Tokyo where his main focus was antimicrobial agents manufactured through fermentation processes. Also in the mid-1950s Umezawa discovered kasugamycin, a compound useful in combating rice molds. In the early 1960s he discovered the cancer drug bleomycin. The Hamao Umezawa Memorial Museum in Setagaya, Tokyo was named in his honour.
Asahi Prize 1958
Paul Ehrlich and Ludwig Darmstaedter Prize 1980
Bristol-Myers Squibb Smissman Award, 1983
David W. Cushman earned his Ph.D. in Biochemistry from the University of Illiois. He then joined the Squibb Institute for Medical Research, where he spent his entire career. Cushman and his colleague, Miguel Ondetti, employed rational design to produce the first ACE inhibitor, captopril.
Cushman and Ondetti shared the 1982 GlaxoSmithKline Alfred Burger Award in Medicinal Chemistry. They also shared the 1999 Albert Lasker Award for Clinical Medical Research and were named "Heroes of Chemistry" by the American Chemical Society.
Miguel Ondetti earned his Ph.D. from the University of Buenos Aires. In 1960 he joined the Squibb Institute for Medical Research, where he spent his entire career. Ondetti and his colleague, David Cushman, employed rational design to produce the first ACE inhibitor, captopril.
Ondetti and Cushman shared the 1982 GlaxoSmithKline Alfred Burger Award in Medicinal Chemistry. They also shared the 1999 Albert Lasker Award for Clinical Medical Research and were named "Heroes of Chemistry" by the American Chemical Society. In 1991 Ondetti was awarded the Perkin Medal.
Bengt I. Samuelsson
The Nobel Prize in Physiology or Medicine 1982
Adapted from the Les Prix Nobel/Nobel Lectures: The Nobel Prizes 1982, Editor Wilhelm Odelberg, [Nobel Foundation], Stockholm, 1983
Bengt Samuelsson was born in Halmstad, Sweden, on May 21, 1934 to Anders and Kristina Samuelsson. After attending public schools he studied medicine at the University of Lund where he met his wife Karin. They have one son (Bo) and two daughters (Elisabet and Astrid). After a few years in Lund he moved to Karolinska Institutet in Stockholm in order to do graduate work in biochemistry in parallel with medical studies. In 1960 he finished his dissertation and became docent in medical chemistry. A year later he also obtained an MD degree from Karolinska Institutet. After a year as research fellow in the Department of Chemistry at Harvard University, he returned to Karolinska Institutet. In 1967 he was appointed professor of medical chemistry at the Royal Veterinary College in Stockholm, and after a few years moved back to Karolinska Institutet to become professor and chairman of the department of physiological chemistry. Concurrently with his research positions he also held administrative posts. He was dean of the medical faculty from 1978 to 1983, and is presently rector of Karolinska Institutet. His research interests were originally in cholesterol metabolism with emphasis on reaction mechanisms. After the structural work on prostaglandins with Sune Bergström in 1959-1962 he has mainly been interested in transformation products of arachidonic acid. This led to the discovery of endoperoxides, thromboxanes and the leukotrienes, and his group has mainly been involved in studying the chemistry, biochemistry and biology of these compounds and their role in biological control systems. This research has implications in several clinical areas, particularly in thrombosis, inflammation and allergy.
Memberships, Awards and Honors
Professor & Head of the Medical Chemistry Department within the Australian National University in Canberra
Adrien Albert was born in Australia and went to London to earn his Ph.D. in 1937. He returned to Australia in 1938, taking a position at Sydney University. During World War II, he worked on synthesis of the antimalarial drug mepacrine and the antiseptic proflavine.
After a brief period at the Wellcome Research Institutio in London, Albert returned to Australia, as Professor and Head of the Medical Chemistry Department within the Australian National University in Canberra. He is well known for his work in heterocycles and the determination of their ionization constants. He was a Fellow of the Australian Academy of Science.
Professor Albert was the 1981 winner of the Bristol-Myers Squibb Smissman Award.
A detailed biography can be found at
Led the chemical research for the discovery of the H2-receptor histamine antagonists
Dr. C. Robin Ganellin was born in London, UK, and received a first class BSc in chemistry from Queen Mary College, University of London, and a PhD in 1958 in organic chemistry with Prof. Michael Dewar for research on tropylium chemistry. During this time he also collaborated with Dr. Rowland Pettit and discovered the oxidative rearrangement of cyclooctatetraene to the tropylium cation. He was a Research Associate in 1960 with Prof. A.C. Cope at MIT, where he devised the first direct optical resolution of chiral olefins using platinum complexes.
He joined Smith Kline & French Laboratories (SK&F) in the UK in 1958 as a medicinal chemist, and from 1966 collaborated with Sir James Black and led the chemical research for the discovery of the H2-receptor histamine antagonists. He was particularly involved in applying principles of physical-organic chemistry to structure-activity analysis. He is coinventor of the drug cimetidine (Tagamet®) which revolutionised the treatment of peptic ulcer disease. He also directed the design of other histamine receptor ligands such as oxmetidine, lupitidine, donetidine, icotidine, zolantidine and temelastine. He was instrumental in establishing the use of the agonists dimaprit and impromidine, and identified compounds for use as chemical controls in histamine pharmacology. He subsequently became Vice-President for Research at the company's Welwyn facility.
In 1986 he was awarded a DSc from London University for his published work on the medicinal chemistry of histamine and drugs acting at histamine receptors and was made a Fellow of the Royal Society. In 1986 he left SK&F and was appointed to the SK&F Chair of Medicinal Chemistry in the Department of Chemistry at University College London (UCL), where he is now Emeritus Professor of Medicinal Chemistry. At UCL his research group have synthesized novel ligands for histamine H3 receptors and he designed the first potent non-imidazole H3-receptor antagonist; He also designed butabindide the first inhibitor of the cholecystokinin-8 inactivating peptidase (tripeptidylpeptidase II). His research has also led to potent blockers (eg UCL 1684, UCL 1848) of the SKCa channel and to ligands for IKCa and BKCa channels. More recently his research has been on Transport-P. He is author or co-author of over 260 scientific publications, has edited 7 books, and is named coinventor on over 160 US patents.
Ganellin has received various international honors, including the UK Royal Society of Chemistry Award for Medicinal Chemistry (1977), their Tilden Medal and Lectureship (1982) and their Adrien Albert Medal and Lectureship (1999), Le Prix Charles Mentzer de France (1978), the ACS Division of Medicinal Chemistry Award (1980), the Society of Chemical Industry Messel Medal (1988), and the Society for Drug Research Award for Drug Discovery (1989). He has also been inducted into the US National Inventors Hall of Fame (1990). He was elected as a Fellow of Queen Mary and Westfield College, London University, (1992) and awarded an Honorary DSc by Aston University in 1995. He received the Nauta Prize on Pharmacochemistry from the European Federation for Medicinal Chemistry (2004), the Pratesi Gold Medal from the Med. Chem. Division of the Societa Chimica Italiana (2006) and was appointed Corresponding Academician to the National Royal Academy of Pharmacy, Spain (2006).
Robin Ganellin belongs to 9 scientific societies (ACS since 1966) and has served on 16 editorial boards or journal advisory committees. He has been visiting Professor of Medicinal Chemistry at the University of Kent at Canterbury (1979-89), Advisory Tutor in Chemistry at the Polytechnic of North London (1979-83) and Director of the Upjohn Discovery Unit at UCL (1987-94). He initiated the biennial RSC Summer School in Medicinal Chemistry in 1981 in the format that exists to date and, indeed, is still lecturing on them. He was a member of the IUPHAR Committee for Receptor Nomenclature and Drug Classification (1990-1998). He is a past Chairman of the Society for Drug Research (1985-87), was President of the Medicinal Chemistry Section of IUPAC (1999-2001), and since 2002 has been Chair of the IUPAC Subcommittee on Medicinal Chemistry and Drug Development.
Tsung Ying Shen was the first winner of the Alfred Burger Award. During his career he was associated with Merck Research Laboratories and the University of Virginia. He was involved in the discovery of indomethacin, as well as inhibitors of platelet activating factor.
Adjunct professor at the department of pharmacology & toxicology of the Medical College of Virginia at Virginia Commonwealth University
From: Chemical and Engineering News, 2008, 86 (39), 53-54.
Born in Timberville, Va., May earned an undergraduate degree from Bridgewater College in 1935 and a Ph.D. in organic chemistry from the University of Virginia in 1939.
After a short stint at National Oil Products, May joined the National Institutes of Health as an associate chemist in 1941. At NIH he served as a senior chemist from 1947 to 1953. While working in the Public Health Service Commissioned Corps., from 1953 to 1977, he was scientist director and then chief of the section on medicinal chemistry.
When May retired in 1977, he joined the department of pharmacology and toxicology of the Medical College of Virginia at Virginia Commonwealth University as an adjunct professor and maintained an active role at the university until shortly before his death.
Early in his career, May focused on antimalarials research, which led to a number of effective drugs. After World War II, he focused on analgesics, introducing the 6,7-benzomorphans and the 5-phenylmorphans as analgesics and research tools. He discovered phenazocine, an opioid analgesic drug, and levomethadyl acetate, which had some success as a replacement for methadone as a maintenance drug in the treatment of opioid addiction. His extensive structure-activity studies emphasized the importance of stereochemistry on drug action and played an important role in the discovery of opioid receptors and the endogenous opioid system. More recently, May made important contributions to the fields of cannabinoids and nicotine.
He served as a board member and a consultant for the National Academy of Sciences Committee on Problems of Drug Dependence, a consultant to the United Nations Narcotics Laboratory, in Vienna, Austria, and a member of the World Health Organization Expert Advisory Panel on Addiction-Producing Drugs. He had been assistant editor of the Journal of Medicinal Chemistry and served on the editorial boards of Medicinal Chemistry Research and Medicinal Research Reviews.
May authored or coauthored 198 research papers, 10 review articles, and seven book chapters. He coedited one book and held seven patents. He received numerous awards, including the Nathan B. Eddy Memorial Award and three awards from ACS: the Hillebrand Prize of the Chemical Society of Washington, the Smissman Bristol-Myers Squibb Award of the Medicinal Chemistry Division, and the Alfred Burger Award in Medicinal Chemistry, a national award. He was a member of ACS, joining in 1940.
Research Fellow in the laboratory of Nobel Prize winner Lavoslav (Leopold) Ruzicka at the ETH in Zurich
Leo Sternbach was born in what is now Croatia. He earned his M. Pharmacy and Ph.D. in organic chemistry from the Jagiellonian University of Karkow, Poland, in 1931. Sternbach was a Research Fellow in the laboratory of Nobel Prize winner Lavoslav (Leopold) Ruzicka at the ETH in Zurich for several years. He was employed by Hoffmann-LaRoche from 1940 until he retired in 1973. He is best known for the discovery of chlordiazepoxide (Librium) and diazepam (Valium).
Sternbach held over 240 patents. He was the 1978 winner of the ACS Division of Medicinal Chemistry Award. In 1979 he won the Chemical Pioneer Award from the American Institute of Chemists. He is also a member of the New Jersey Inventors Hall of Fame and the National Inventors Hall of Fame.
Alfred Burger was born on September 6, 1905, in Vienna, Austria-Hungary (now Austria), the son of S. L. Burger (a civil servant) and Clariss Burger. After receiving his Ph.D. in chemistry from the University of Vienna and conducting postdoctoral research in Switzerland in 1928, Burger immigrated to the United States the following year. On August 1, 1936, he married Frances Page Morrison, who eventually bore him one daughter, Frances. In 1937, Burger became a naturalized citizen of the United States.Upon arrival in the United States in 1929, Burger went to work as a research associate at the newly created Drug Addiction Laboratory at the University of Virginia. Throughout his long research career, he remained linked to the University. Burger's work, which focused on laboratory research from 1929-1938, later included teaching. An assistant professor from 1938-1939, Burger was an associate professor from 1939-1952, when he was promoted to full professor, a position he held until 1970, acting as department chair from 1962-1963. In 1970, he was named Professor Emeritus.
Burger's entire career has been devoted to studying chemicals and their medicinal properties. As an expert in organic chemistry he pinpointed the syntheses of morphine substitutes, and also researched and designed numerous drugs, including antimalarials, antituberculous drugs, organic phosphorous compounds, antimetabolites, and psychopharmacological drugs. He also did much to further chemotherapy, acting as a member of the chemistry panel and then as a medical chairman of the Cancer Chemotherapy National Service Center from 1956 through 1964. His most recent work focused on monoamine oxidase (MAO) inhibitors and antidepressant drugs.
In 1958, Burger founded the Journal of Medicinal Chemistry, providing a formal communication venue for his discipline. He was editor of the Journal from its inception through 1971. Today, the journal still remains a voice for medicinal chemist from around the globe.
Burger's scientific accomplishments did not go unnoticed by his peers. In 1953, he was awared the Pasteur Medal by the Pasteur Institute in Paris. In 1971, he received an honorary degree from the Philadelphia College of Pharmacy and Science, as well as an award from the American Pharmacological Society Foundation. In 1977, The American Chemical Society recognized his contribution to medicinal chemistry by giving him the Smissman Award. Burger received his greatest accolade when the American Chemical Society created the Alfred Burger Award in Medicinal Chemistry in his honor.
Burger was a long-time member of the American Chemical Society and the American Pharmacological Society. A prolific writer, he published nine books, as well as about 200 peer-reviewed articles.
Bernard Belleau was responsible for the discovery of lamivudine (3TC), a nucleoside analog inhibitor of viral reverse transcriptase. He earned B.Sc. and M.Sc. degrees from the Université de Montréal, and his Ph.D. from McGill University. His career included positions at the University of Ottawa, McGill University, Bristol Laboratories, and BioChem Pharma. Belleau won the ACS Division of Medicinal Chemistry Award in 1976. He was inducted into The Canadian Medical Hall of Fame in 2000.
Corwin Hansch, the founder of the QSAR discipline was born on October 6, 1918, in Kenmare, North Dakota. He started his studies at Lincoln College, in 1936-37, worked on his B.S. at the University of Illinois, from 1937 - June 1940 and his Ph.D. at New York University, from 1940 - January 1944. From January 1944 - July 1944, he was a postdoc at the University of Illinois, Chicago. From July 1944 - October 1944, he worked on the Manhattan Project at the University of Chicago. From November 1944 - October 1945, he was active as a group leader on the Manhattan Project, at du Pont de Nemours, in Richland. From October 1945 - February 1946, he was a Research Chemist at du Pont de Nemours, in Wilmington, Delaware. In February 1946, he joined Pomona College, Claremont, where he is still active today. During this time he spent a sabbatical year at the ETH in Zurich, in 1952, and another sabbatical year at Huisgen's lab, in Munich, in 1959. Whereas his first field of research was high temperature dehydrogenation, early on he changed to correlations of biological activity with chemical structure. Corwin Hansch initiated the field of quantitative structure-activity relationships in the years 1962 and 1963 with these seminal publications: C. Hansch, P. P. Maloney, T. Fujita and R. M. Muir, Correlation of Biological Activity of Phenoxyacetic Acids with Hammett Substituent Constants and Partition Coefficients, Nature 1962, 194, 178-180; C. Hansch, R. M. Muir, T. Fujita, P. P. Maloney, C. F. Geiger and M.Streich, The Correlation of Biological Activity of Plant Growth-Regulators and Chloromycetin Derivatives with Hammett Constants and Partition Coefficients, J. Amer. Chem. Soc. 1963, 85, 2817-2824. In 1964, he published two additional papers that are considered to be the key references for the development of the Hansch Analysis, as it is now called, and for the calculation of partition coefficients from lipophilicity constants. He has earned numerous honours and awards, including the Smissman-Bristol Award in Medicinal Chemistry from the ACS in 1976, and an honorary professorship from the University of Beijing. His papers are citation classics and for several years he was one of the 300 most cited authors, out of 1 million scientists, active in all different fields of research. He has more than 300 publications as well asa number of books Several books by other authors have been dedicated to Corwin Hansch, in honor of his contributions to science.
Josef Fried was born in Poland in 1914 and came to the United States in 1938 to study at Columbia University. There he earned his Ph.D. in 1940 and did postdoctoral work until 1943. In 1944 he joined the Squibb Institute for Medical Research, where he did pioneering work in fluorinated corticosteroids. He moved to the University of Chicago in 1963 and did seminal work on the synthesis of prostaglandins. He won the American Chemical Society's Medicinal Chemistry Award in 1974. Fried was a member of the National Academy of Sciences.
Adapted from an article in the University of Chicago Chronicle
George Hitchings earned his B.S. degree in chemistry from the University of Washington in 1927, and his Ph.D. from Harvard University in 1933. He spent a number of years at Western Reserve University (now Case Western Reserve), and in 1942 he joined Wellcome Research Laboratories in Tuckahoe, New York. There, he and his colleagues discovered pyrimethamine (antimalarial), 6-mercaptopurine and thioguanine (anti-leukemic), and trimethoprim (antibacterial). In 1988, he shared the Nobel Prize in Physiology or Medicine with Gertrude Elion (also a member of the Medicinal Chemistry Hall of Fame) and James Black.
Adapted from Hitchings' Nobel Prize biography
James M. Sprague received his AB at Franklin College in 1930 and his PhD at the University of Wisconsin, Madison with Homer Adkins in 1934, studying the hydrogenation and hydrogenolysis of diketones. He then did postdoctoral work at Yale, and started at Sharpe and Dohme in 1937, and then continued at Merck Sharpe and Dohme when the two companies merged in 1953. Sprague worked extensively in the area of heterocyclic compounds, and was responsible for 27 United States patents and several foreign patents for the Merck Co., Inc. He made important discoveries in the area of sulfa drugs, which initially became important as the first effective antimicrobial drugs, but later found broader uses. Particularly important was the development of a new class of drugs, the thiazide diuretics. One of these, the drug Diuril®, dramatically altered the treatment of congestive heart failure and high blood pressure. Other products he helped develop are Elavil®, an antidepressant, and Benemid®, a treatment for gout. Sprague died in 2000 at the age of 91.
The Merck Lectureship in honor of Sprague started in 1959 at the University of Wisconsin. The first speaker was George Wittig, who later won the Nobel prize, and subsequently the Lectureship was awarded to three other chemists (Donald J. Cram, Derek H. Barton and Robert Grubbs) who went on to win Nobel Prizes in chemistry.
Sydney Archer was born in New York City on January 23, 1917. He earned his baccalaureate degree in chemistry at the University of Wisconsin in 1937 and received his PhD in organic chemistry in 1940 from Pennsylvania State University under the direction of J. H. Simons. Following postdoctoral appointments at Northwestern and University of Chicago, and a brief period of employment at the Sun Oil Co., Sydney Archer joined the Sterling-Winthrop Research Institute in East Greenbush, NY in 1943 where, during his 30 years of employment, he attained the position of Vice President. It is rare for a medicinal chemist to put his or her thumbprint on a molecule that is marketed to treat human disease. Sydney Archer’s thumbprint is on many; these include the analgesic talwin, hycanthone for the treatment of schistosomiasis, a tropical disease, and telepaque, an X-ray contrast agent.
His association with Rensselaer began in 1961 with his appointment as Adjunct Professor of Chemistry with responsibility for teaching medicinal chemistry. Upon his retirement from Sterling-Winthrop in 1973, Dr. Archer assumed his second illustrious career in medicinal chemistry as Research Professor of Medicinal Chemistry at Rensselaer. His record of accomplishment continued at Rensselaer. His interests in the treatment of drug addiction led the way to the founding of the NYS Capital District Center for Drug Abuse Research and Treatment. Institutions involved in this effort include Rensselaer, Albany Medical College and the SUNY School of Public Health. The center is unique in an academic environment in that its membership has expertise at all levels necessary to confront the problems of drug abuse from the synthetic chemistry laboratory to the clinic. At the time of his death, Sydney Archer was still extremely active and provided great leadership to drug addiction research programs at the local, state, national, and international levels. He started and maintained research collaborations in this field and others with distinguished scientists throughout the world. His work at Rensselaer was backed by major funding from the National Institutes of Health and the National Institute on Drug Abuse.
During the period 1980-85, Dr. Archer served Rensselaer as Dean of the School of Science. Under his leadership, Rensselaer launched the highly successful School of Science Initiative.
Dr. Archer has served on numerous public service committees dedicated to fostering human health worldwide. He has authored over 150 journal articles and holds over 100 US Patents. In 1980, he was awarded the prestigious Medicinal Chemistry Award sponsored by the American Chemical Society. In recognition of these and other scientific and professional accomplishments, Rensselaer instituted the Archer Lecture Series in Organic and Medicinal Chemistry in 1985, endowed by Sterling-Winthrop. The excellence of the Archer Lecture speakers to date is a true testimony to the excellence of Sydney Archer.
Adapted from a biography of Sidney Archer by Mark Wentland
Professor B.R. Baker served as Professor of Chemistry at UCSB from 1966 until his death in 1971. Baker's graduate work on the structural elucidation and synthesis of Cannabis constituents marked the beginning of a prolific career in the chemistry of natural products. He undertook many diverse projects of medicinal interest including the synthesis of antihemorrhagic vitamin K analogues, biotin derivatives, compounds with hormone activity, sulfones with activity against tuberculosis, and alkaloids. He published two books and more than 370 papers that included a series of papers on the structure and synthesis of the antimalarial alkaloid from Hydrangea, febrifugine, that filled an entire issue of the Journal of Organic Chemistry in 1952. He determined the structure of the first known nucleoside antibiotic, puromycin, and synthesized it in 1955. This achievement came long before the discovery of the structure of transfer ribonucleic acid (tRNA). Puromycin was later shown to mimic the structure of tRNA and became and an important tool for research in molecular biology. Puromycin was too toxic for cancer chemotherapy, but it aroused Baker's interest in this field. Few of the myriad of compounds that he had so meticulously synthesized showed any antitumor activity in vivo, so he sought a more rational approach to cancer chemotherapy. Perhaps his greatest contribution to medicinal chemistry was the concept of active-site-directed irreversible enzyme inhibition of substrate-identical enzymes. A monograph summarizing this approach to drug design promptly became on of the classic works in the field.
Adapted from http://www.chem.ucsb.edu/seminars/baker.php