Division of Medicinal Chemistry

Hall of Fame

(For a brief history of the Division, CLICK HERE)

The ACS Division of Medicinal Chemistry Hall of Fame was established by the executive committee of the Division in 2006. Inductees must be members of the Division who have made an overall outstanding contribution to medicinal chemistry through a combination of research, teaching and service, but whose efforts in any of these individual catagories has not yet qualified them for one of the national ACS or Division awards (see below). Up to three scientists will be inducted into the Hall of Fame each calendar year, and the inductees will be recognized at a reception at the Fall national meeting of the American Chemical Society. Those honored by Hall of Fame membership are not excluded from receiving the traditional Division awards described below, and recipients of the Smissman, Division of Medicinal Chemistry, Burger and Hershberg awards are automatically added to the Hall of Fame roster. Please scroll down for a list of these previous award recipients.

2007 Division of Medicinal Chemistry Hall of Fame Inductees

Burton G. Christensen, Ph.D.

Dr. Burton G. Christensen was born in Waterloo, Iowa on 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 position 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 beta-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 1-alpha 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 5-alpha 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.

James K. Coward, Ph.D. is Professor of Medicinal Chemistry and Professor of Chemistry at the 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. His 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 methylthio-adenosine. Second-generation inhibitor synthesis was aimed at “multisubstrate adduct” inhibitors of catechol O-methyl-transferase, spermidine synthase (AdoDATO, AdoSpd), and spermine synthase (AdoDATAD). In related research, a series of alpha 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-gamma glutamate derivatives of reduced folates and antifolates are catalyzed by folylpoly-gamma glutamate synthetase, an ATP-dependent ligase, and gamma 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 (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 65 graduate students and postdoctoral associates, as well as over 50 undergraduate students. He is a Fellow, Chemistry Section, American Association for the Advancement of Science (2004).

Robert Vince, Ph.D.

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 Universuty 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.

Kenner Rice, Ph.D.
2007 Bristol-Myers Squibb Smissman Awardee

Dr. Kenner Rice, Chief of the Chemical Biology Research Branch of the National Institute on Drug Abuse, NIH will receive the 2007 Smissman Award, sponsored by Bristol-Myers Squibb. He will receive this award in the Division of Medicinal Chemistry at the 234th ACS National Meeting in Boston, on Monday, August 20, 2007. 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 non-narcotic 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.

2006 Hall of Fame Inductees

Division Awards in Medicinal Chemistry

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