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Toomas Mitt

Bristol-Myers Squibb

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Featured researches published by Toomas Mitt.

Bioorganic & Medicinal Chemistry Letters | 2002

Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase.

Edwin J. Iwanowicz; Scott H. Watterson; Chunjian Liu; Henry H. Gu; Toomas Mitt; Katerina Leftheris; Joel C. Barrish; Catherine A. Fleener; Katherine A. Rouleau; N.Z. Sherbina; Diane Hollenbaugh

A series of novel guanidine-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.

Bioorganic & Medicinal Chemistry Letters | 1995

α-hydroxyamide derived aminodiols as potent inhibitors of hiv protease

Saleem Ahmad; Aaila Ashfaq; Masud Alam; Gregory S. Bisacchi; Ping Chen; Peter T. W. Cheng; Jill A. Greytok; Mark A. Hermsmeier; Pin-Fang Lin; Karen A. Lis; Zoeb Merchant; Toomas Mitt; Mark T. Skoog; Steven H. Spergel; Joseph A. Tino; Gregory D. Vite; Richard J. Colonno; Robert Zahler; Joel C. Barrish

Abstract A novel series of HIV protease inhibitors has been prepared. Replacement of the P2 carbamate of compound 1 [IC50 = 125 nM] with an α-hydroxy amide moiety results in a significant increase in anti-HIV protease activity [e. g., compound 25a; IC50 = 15 nM]. Furthermore, isomers with (R) absolute configuration at the P2 site show greater inhibitory activity than the corresponding (S)-isomers. A proposed binding mode based on molecular modeling is used to rationalize the structure-activity relationships.

Journal of Medicinal Chemistry | 2002

Discovery of Aminothiazole Inhibitors of Cyclin-Dependent Kinase 2: Synthesis, X-Ray Crystallographic Analysis, and Biological Activities

Kyoung S. Kim; S. David Kimball; Raj N. Misra; David B. Rawlins; John T. Hunt; Hai-Yun Xiao; Songfeng Lu; Ligang Qian; Wen-Ching Han; Weifang Shan; Toomas Mitt; Zhen-Wei Cai; Michael A. Poss; Hong Zhu; John S. Sack; John S. Tokarski; Chieh Ying Chang; Nikola P. Pavletich; Amrita Kamath; William G. Humphreys; Punit Marathe; O Isia Bursuker; Kristen A. Kellar; Urvashi V. Roongta; Roberta Batorsky; Janet G. Mulheron; David K. Bol; Craig R. Fairchild; and Francis Y. Lee; Kevin R. Webster

Journal of Medicinal Chemistry | 2000

Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.

John T. Hunt; Charles Z. Ding; Roberta Batorsky; Mark S. Bednarz; Rajeev S. Bhide; Young H. Cho; Saeho Chong; Sam T. Chao; Johnni Gullo-Brown; Peng Guo; Soong Hoon Kim; Francis Y. Lee; Katerina Leftheris; Arthur V. Miller; Toomas Mitt; Manorama Patel; Becky Penhallow; Carol Ricca; William C. Rose; Robert J. Schmidt; William Allen Slusarchyk; Gregory D. Vite; Veeraswamy Manne

Journal of Medicinal Chemistry | 2004

Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.

John T. Hunt; Toomas Mitt; Robert M. Borzilleri; Johnni Gullo-Brown; Joseph Fargnoli; Brian E. Fink; Wen-Ching Han; Steven Mortillo; Gregory D. Vite; Barri Wautlet; Tai Wong; Chiang Yu; Xiaoping Zheng; Rajeev S. Bhide

Journal of Medicinal Chemistry | 1991

Synthesis and antiviral activity of enantiomeric forms of cyclobutyl nucleoside analogs

Gregory S. Bisacchi; Abbe Braitman; Christopher Cianci; Junius M. Clark; A.Kirk Field; Moira Hagen; Deborah R. Hockstein; Mary F. Malley; Toomas Mitt

Archive | 2002

Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function

Mark E. Salvati; James Aaron Balog; Dacia A. Pickering; Soren Giese; Aberra Fura; Wenying Li; Ramesh N. Patel; Ronald L. Hanson; Toomas Mitt; Jacques Y. Roberge; James R. Corte; Steven H. Spergel; Richard Rampulla; Raj N. Misra; Hai-Yun Xiao

Journal of Medicinal Chemistry | 1999

Discovery and Structure−Activity Relationships of Imidazole-Containing Tetrahydrobenzodiazepine Inhibitors of Farnesyltransferase.

Charles Z. Ding; Roberta Batorsky; Rajeev S. Bhide; Chao Hj; Young H. Cho; Chong S; Johnni Gullo-Brown; Peng Guo; Kim Sh; Francis Y. Lee; Katerina Leftheris; Arthur V. Miller; Toomas Mitt; Manorama Patel; Becky Penhallow; Carol Ricca; William C. Rose; Robert J. Schmidt; William Allen Slusarchyk; Gregory D. Vite; Ning Yan; Manne; John T. Hunt

Bioorganic & Medicinal Chemistry Letters | 2005

New dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Brian E. Fink; Gregory D. Vite; Harold Mastalerz; John F. Kadow; Soong-Hoon Kim; Kenneth J. Leavitt; Karen Du; Donald Crews; Toomas Mitt; Tai W. Wong; John T. Hunt; Dolatrai M. Vyas; John S. Tokarski

Journal of Organic Chemistry | 1995

Regioselective Coupling of Tetraalkylammonium Salts of 6-Iodo-2-aminopurine to a Cyclobutyl Triflate: Efficient Preparation of Homochiral BMS-180,194, a Potent Antiviral Carbocyclic Nucleoside

Gregory S. Bisacchi; Janak Singh; Jollie D. Godfrey; Thomas P. Kissick; Toomas Mitt; Mary F. Malley; John D. Di Marco; Jack Z. Gougoutas; Richard H. Mueller; Robert Zahler

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Collaboration

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Gregory S. Bisacchi

Bristol-Myers Squibb

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John T. Hunt

Princeton University

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Gregory D. Vite

Bristol-Myers Squibb

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Janak Singh

Loyola University New Orleans

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Jollie D. Godfrey

Princeton University

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Katerina Leftheris

Bristol-Myers Squibb

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Richard H. Mueller

Yale University

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Robert Zahler

Harvard University

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Thomas P. Kissick

Princeton University

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Rajeev S. Bhide

University of Wisconsin-Madison

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