R
Raj N. Misra
Researcher at Bristol-Myers Squibb
Publications - 41
Citations - 1698
Raj N. Misra is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: Cyclin-dependent kinase & Protein kinase A. The author has an hindex of 21, co-authored 41 publications receiving 1642 citations.
Papers
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Journal ArticleDOI
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.
Raj N. Misra,Hai-Yun Xiao,Kyoung S. Kim,Songfeng Lu,Wen-Ching Han,Stephanie Barbosa,John T. Hunt,Rawlins David B,Weifang Shan,Syed Z. Ahmed,Ligang Qian,Bang-Chi Chen,Rulin Zhao,Mark S. Bednarz,Kristen A. Kellar,Janet G. Mulheron,Roberta Batorsky,Urvashi V. Roongta,Amrita Kamath,Punit Marathe,Sunanda A. Ranadive,John S. Sack,John S. Tokarski,Nikola P. Pavletich,Francis Y. Lee,Kevin R. Webster,S. David Kimball +26 more
TL;DR: Ncyl-2-aminothiazoles with nonaromatic acyl side chains containing a basic amine were found to be potent, selective inhibitors of CDK2/cycE which exhibit antitumor activity in mice.
Journal ArticleDOI
Dual Metalloprotease Inhibitors: Mercaptoacetyl-Based Fused Heterocyclic Dipeptide Mimetics as Inhibitors of Angiotensin-Converting Enzyme and Neutral Endopeptidase
Jeffrey A. Robl,Chongqing Sun,Jay Stevenson,Denis E. Ryono,Ligaya M. Simpkins,Maria P. Cimarusti,Tamara Dejneka,William A. Slusarchyk,Sam T. Chao,Leslie Stratton,Raj N. Misra,Mark S. Bednarz,M. M. Asaad,Hong Son Cheung,B.E. Abboa-Offei,Patricia L. Smith,Parker D. Mathers,Maxine Fox,T. R. Schaeffer,and Andrea A. Seymour,Nick C. Trippodo +20 more
TL;DR: A series of 7,6- and 7,5-fused bicyclic thiazepinones and oxazepinones were generated and incorporated as conformationally restricted dipeptide surrogates in mercaptoacyl dipePTides, and compound 1a (BMS-186716) was advanced into clinical development for the treatment of hypertension and congestive heart failure.
Journal ArticleDOI
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,Rawlins David B,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,Isia Bursuker,Kristen A. Kellar,Urvashi V. Roongta,Roberta Batorsky,Janet G. Mulheron,David Bol,Craig R. Fairchild,Francis Y. Lee,Kevin R. Webster +29 more
TL;DR: Optimization led to compounds such as water soluble 45, which possesses a favorable pharmacokinetic profile in mice and demonstrates significant antitumor activity in vivo in several murine and human models, including an engineered murine mammary tumor that overexpresses cyclin E, the coactivator of CDK2.
Patent
Aminothiazole inhibitors of cyclin dependent kinases
Kyoung S. Kim,S. David Kimball,Zhen-Wei Cai,Rawlins David B,Raj N. Misra,Michael A. Poss,Kevin R. Webster,John T. Hunt,Wen-Ching Han +8 more
TL;DR: The symbols have the following meanings: R1 and R2 are independently hydrogen, fluorine or alkyl; R3 is aryl or heteroaryl.
Journal ArticleDOI
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.
Kyoung S. Kim,John S. Sack,John S. Tokarski,Ligang Qian,Sam T. Chao,Leslie Leith,Y. F. Kelly,Raj N. Misra,John T. Hunt,Kimball Sd,William G. Humphreys,Barri Wautlet,Janet G. Mulheron,K R Webster +13 more
TL;DR: CDK1 selective thio- and oxoflavopiridol analogues inhibit the colony-forming ability of multiple human tumor cell lines and possess a unique antiproliferative profile in comparison to flavopirodol.