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Lester Mitscher Research

  • B.S. 1953, Wayne University
  • Ph.D. 1958, Wayne State University

Awards / Honors

  • Award in Medicinal Chemistry, Division of Medicinal Chemistry, ACS - 2000
  • Elected Fellow, International Union of Pure and Applied Chemistry - 2002
  • Research Achievement Award, American Society for Pharmacognosy - 2007
  • Selected Member Medicinal Chemistry Hall of Fame, Medicinal Chemistry Division, American Chemical Society - 2007
  • Elected Fellow, American Society for Pharmacognosy - 2007
  • International Union of Pure and Applied Chemistry Distinguished Fellow Award - 2009

U.S. PATENTS (Related foreign patents not listed)

  • J. D. Albright, L. A. Mitscher, L. Goldman. New derivatives of yohimbe alkaloids. Belg. 611,137 (1962).CA 60:P 14557d (1964).
  • P. A. Miller, J. H. E. J. Martin, L. A. Mitscher. Novel 5a,6-Anhydrotetracyclines. US 3,265,732 (1966). CA 66:P1587a (1967).
  • S. E. DeVoe, L. A. Mitscher. Antibiotic RA-6950beta and method of production using Streptomyces ochrosporus. U.S. 3,177,243 (1968).
  • L. A. Mitscher, J. H. E. J. Martin. Isolation of 5-hydroxy-7-chlortetracycline. U. S. 3,446,841 (1969). CA 71:P 38667b (1969).
  • J. H. Martin, J. N. Porter, L. A. Mitscher. Antibiotic AF283 from Streptomyces. U.S. 3,452,136 (1969).CA 71:P 59640c (1969).
  • M. P. Kunstmann, L. A. Mitscher, J. N. Porter. Antibiotic neutramycin by fermentative biosynthesis with Streptomyces deuteoverticillatus. U.S. 3,549,502 (1970). CA 74: P110418c (1971).
  • W. J. McGahren, L. A. Mitscher, J. N. Porter. Antifungal agents by cultivating Sporormia affinis, U.S. 3,555,075 (1971). CA 75:P 18626s (1971).
  • L. A. Mitscher, G. W. Clark, III, G. H. Bokelman. Prostaglandin intermediates from a mould metabolite. U.S. 4,103,091 (1978). CA 90:P 71825s (1979).
  • L. A. Mitscher, G. W. Clark, G. H. Bokelman. Intermediates for the preparation of prostaglandins and prostaglandin analogs from a mould metabolite. U.S. 4,188,329 (1980).
  • L. A. Mitscher, G. W. Clark, III, P. B. Hudson. Intermediate for prostaglandins and process for preparing the intermediate. U.S. 4,229,592 (1980).
  • J. Alexander, L. A. Mitscher. Anathracycline synthesis. U.S. 4,224,880 (1981).
  • L. A. Mitscher. Anthracycline synthesis. U.S. 4,215,062 (1980). CA 94:P 15447r (1981).
  • L. A. Mitscher. Regiospecific syntheses of anthracyclinone compounds such as daunomycinone. U.S. 4,374,979 (1983).
  • L. A. Mitscher. Anthracycline synthesis. U.S. 4,405,522 (1983). CA 100:P 22435f(1984).
  • L. A. Mitscher, D. Lednicer. Biosynthesis of simplified anthracyclines. U.S. 4,471,052 (1984). CA102:P 22797s (1985).
  • L. A. Mitscher, D. T. W. Chu. Process for preparation of racemic and optically active ofloxacin and related derivatives. U.S. 4,777,253 (1988). CA 110:P 75530w (1989).
  • L. A. Mitscher, D. T. Chu. Intermediates for preparation of racemate and optically active ofloxacin and related derivatives. U.S. 4,826,985 (1989).
  • W. R. Baker and L. A. Mitscher. Isoflavonoid antibacterial compounds, compositions and use. U.S.5,399,558 (1995).
  • W. R. Baker and L. A. Mitscher. Indolo[2,1-biquinazoline-6,12-dione antibacterial compounds and methods of use thereof. U.S. 5,441,955 (1995).
  • L. A. Mitscher, Stabilized aqueous steroid immunoassay standards with cyclodextrins. U.S. 5,679,573 (1997).

Elective National Offices Held

  • Vice Chairman, Medicinal Chemistry Division, American Chemical Society 1972-1973
  • Chairman, Medicinal Chemistry Division, American Chemical Society 1973-1974
  • Councillor, Medicinal Chemistry Division, American Chemical Society 1978-1982
  • Vice Chairman, American Society for Pharmacognosy 1991-1992
  • Chairman, American Society for Pharmacognosy 1992- 1993

Editorships

  • Allergy and Infectious Diseases 1968-1971
  • Antimicrobial Agents and Chemotherapy 1971-1974
  • The Journal of Antibiotics 1973-date
  • Heterocycles 1973-date
  • Saudi Journal of Pharmaceutical Sciences 1992-date
  • The Journal of Medicinal Chemistry 1994-1999
  • Bioorganic & Medicinal Chemistry Letters 1994-1999
  • Bioorganic & Medicinal Chemistry 1994-1999
  • The Journal of Natural Products 1995-1999
  • Combinatorial Chemistry & High Throughput Screening 1997-date
  • Medicinal Research Reviews (Editor-in-Chief) 1996-1998
  • Medicinal Research Reviews (Contributing Editor) 1998-date
  • Molecules Online 1997-2000
  • Current Drugs Advisory Board 1998-date
  • Current Drug Targets - Inflammation and Allergy 2000-2002
  • Natural Product Letters 2002-date
  • Current Drug Discovery Techniques 2002-date
  • Natural Products Research 2004-date
  • Bioactive Natural Products 2005-date
  • Journal of Food and Drug Analysis 2000-date

Natural products, antibiotics, antivirals, antimutagenics/ chemopreventive agents, antitumor agents.

The Mitscher group has a long-term interest in the identification through directed screening of pharmacologically active natural products, determination of their structural formulae, evaluation of their therapeutic potential and synthesis (partial and total) of analogues in attempts to improve their therapeutic potential. In the quinolone antibacterial field, his group is exploring the molecular mode of action and resistance mechanisms through synthesis and evaluation against purified enzyme (DNA gyrase) of this important class of drugs.

He is also active in combinatorial chemistry methodologies

Professor Mitscher has received the Smissman Award and Medicinal Chemistry Award (ACS), Research Achievement Award (APhA), Volweiler Award (AACP), the Higuchi-Simons Award (KU), and is an elected Fellow of the American Association for the Advancement of Science. He served as chair of the Department of Medicinal Chemistry from 1975-1993, and has held posts in numerous professional organizations. He consults for several major pharmaceutical firms, and is on the editorial advisory boards of the Journal of Medicinal Chemistry, Heterocycles, the Journal of Antibiotics, Biorganic and Medicinal Chemistry, Biorganic and Medicinal Chemistry Letters, and the Saudi Journal of Pharmaceutical Sciences.

Selected Publications (From a total of 268)

  • E. J. Gentry, H. Telikepalli, P. Srinivas and L. A. Mitscher, Tetraacyldiborates. Selective and efficient acylation reagents suitable for multiple parallel synthetic applications, Combinatorial Chemistry and High Throughput Screening, 2003, 6, 139-145.
  • S. Menon, H. Vaidya, S. Pillai, R. Vidya and L. A. Mitscher, A demonstration library of indazoles containing novel antimutagenic/ antioxidant leads, Combinatorial Chemistry and High Throughput Screening, 2003, 6, 471-480.
  • L. A. Mitscher and R. Cooper, Echinacea and Immunostimulation in Herbal and Traditional Medicine: Molecular Basis of Health, L. Packer, C. N. Ong and B. Halliwell, Eds., 2004, M. Dekker, NY, 721-756.
  • L. A. Mitscher, Contemporary Drug Discovery, in Process Chemistry, M. Chorgade, Ed., 2004, J. Wiley and Sons, Inc., N.Y., in press.
  • L. A. Mitscher, A Modern Look at Folkloric Use of Anti-infective Agents, in Handbook of Medicinal Plants, Z. Yaniv and U. Bachrach, Eds., Haworth Press, Inc., NY., in press.
  • L. A. Mitscher and A. Dutta. "Combinatorial Chemistry" in Burger's Medicinal Chemistry, Sixth Ed., Wiley and Sons, NY, 2003, Vol. 2, 2-36.
  • R. A. Fecik, P. Devasthale, S. Pillai, A. Keschavarz-Shokri, L. Shen and L. A. Mitscher. Chiral DNA Gyrase Inhibitors. 3. Probing the chiral preference of the active site of DNA gyrase. Synthesis of 10-fluoro-6-methyl-6,7-dihydro-9-piperazinyl-2H-benzo[a]quinolizine-2-one-3-carboxylic acid analogs. J. Med. Chem. 2005. 1229-36.
  • Mitscher, L. A. Bacterial topoisomerase inhibitors: quinolone and pyridone antibacterial agents. Chem Rev., 2005, 105, 559-592.
  • J. B. Laursen, J. Nielsen, T. Haack, S. Pusuluri, S. David, R. Balakrishna, Y. Zheng, Z. Ma, T. B. Doyle and L. A. Mitscher. Further exploration of antimicrobial ketodihydronicotinic acid derivatives by multiple parallel syntheses. Comb Chem High Throughput Screen. 2006, 9, 663-681.
  • L. A. Mitscher. Traditional Medicines. In Comprehensive Medicinal Chemistry II, Volume 1, Elsevier, New York, 2006, p405-430.
  • L.A. Mitscher, A. Dutta. Contemporary drug discovery. Drug Disc Dev. 2006, 1, 103-128.
  • S. Pillai, C. Pillai, L.A. Mitscher, R. Cooper. Use of quantitative flow cytometry to measure ex vivo immunostimulant activity of echinacea: the case for polysaccharides. J Alt Comp Med. 2007, 13, 625-634.
  • L.A. Mitscher, T.L. Lemke, E.J. Gentry. Antibiotics and Antimicrobial Agents, in Foye's Principles of Medicinal Chemistry, 6th Edition, Lippincott, Williams & Wilkins, Philadelphia, 2008, p1028-1083.
  • P. Vedantham, M. Zhang, P.J. Gor, M. Huang, G.I. Georg, G.H. Lushington, L.A. Mitscher, Q.-Z. Ye, P.R. Hanson. Studies towards the synthesis of methioinine aminopeptidase inhibitors: diversification utilizing a ROMP-derived coupling reagent. J Comb Chem. 2008, 10, 195-203.
  • L.A. Mitscher. Coevolution: mankind and microbes. J Nat Prod. 2008, 71, 497-509.

Books

  • The Organic Chemistry of Drug Synthesis. D. Lednicer and L. A. Mitscher. 1977, Wiley Interscience, New York, N.Y. Vol. 1.
  • The Organic Chemistry of Drug Synthesis. D. Lednicer and L. A. Mitscher. 1979, Wiley Interscience, New York, N.Y. Vol. 2.
  • The Organic Chemistry of Drug Synthesis. D. Lednicer and L. A. Mitscher. 1984, Wiley Interscience, New York, N.Y. Vol. 3.
  • The Organic Chemistry of Drug Synthesis. D. Lednicer, G. I. Georg and L. A. Mitscher. Wiley Interscience, New York, N.Y. Vol. 4., 1989
  • The Chemistry of the Tetracycline Antibiotics. L. A. Mitscher. Marcel Dekker, New York, N.Y. 1978.
  • The Green Tea Book: China's Fountain of Youth. L. A. Mitscher and Virginia Dolby, Avery Press, N. Y. 1997

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