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Leroy B. Townsend, Ph.D.

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.

ACS Division of Medicinal Chemistry

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