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Page 1
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.
Kim KS, Kimball SD, Misra RN, Rawlins DB, Hunt JT, Xiao HY, Lu S, Qian L, Han WC, Shan W, Mitt T, Cai ZW, Poss MA, Zhu H, Sack JS, Tokarski JS, Chang CY, Pavletich N, Kamath A, Humphreys WG, Marathe P, Bursuker I, Kellar KA, Roongta U, Batorsky R, Mulheron JG, Bol D, Fairchild CR, Lee FY, Webster KR. Kim KS, et al. J Med Chem. 2002 Aug 29;45(18):3905-27. doi: 10.1021/jm0201520. J Med Chem. 2002. PMID: 12190313
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.
Misra RN, Xiao HY, Kim KS, Lu S, Han WC, Barbosa SA, Hunt JT, Rawlins DB, Shan W, Ahmed SZ, Qian L, Chen BC, Zhao R, Bednarz MS, Kellar KA, Mulheron JG, Batorsky R, Roongta U, Kamath A, Marathe P, Ranadive SA, Sack JS, Tokarski JS, Pavletich NP, Lee FY, Webster KR, Kimball SD. Misra RN, et al. J Med Chem. 2004 Mar 25;47(7):1719-28. doi: 10.1021/jm0305568. J Med Chem. 2004. PMID: 15027863
Selective Itk inhibitors block T-cell activation and murine lung inflammation.
Lin TA, McIntyre KW, Das J, Liu C, O'Day KD, Penhallow B, Hung CY, Whitney GS, Shuster DJ, Yang X, Townsend R, Postelnek J, Spergel SH, Lin J, Moquin RV, Furch JA, Kamath AV, Zhang H, Marathe PH, Perez-Villar JJ, Doweyko A, Killar L, Dodd JH, Barrish JC, Wityak J, Kanner SB. Lin TA, et al. Among authors: kamath av. Biochemistry. 2004 Aug 31;43(34):11056-62. doi: 10.1021/bi049428r. Biochemistry. 2004. PMID: 15323564
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM, Fairchild C, Hunt JT, Inigo I, Johnston K, Kamath A, Kan D, Klei H, Marathe P, Pang S, Peterson R, Pitt S, Schieven GL, Schmidt RJ, Tokarski J, Wen ML, Wityak J, Borzilleri RM. Lombardo LJ, et al. J Med Chem. 2004 Dec 30;47(27):6658-61. doi: 10.1021/jm049486a. J Med Chem. 2004. PMID: 15615512
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Bhide RS, Cai ZW, Zhang YZ, Qian L, Wei D, Barbosa S, Lombardo LJ, Borzilleri RM, Zheng X, Wu LI, Barrish JC, Kim SH, Leavitt K, Mathur A, Leith L, Chao S, Wautlet B, Mortillo S, Jeyaseelan R Sr, Kukral D, Hunt JT, Kamath A, Fura A, Vyas V, Marathe P, D'Arienzo C, Derbin G, Fargnoli J. Bhide RS, et al. J Med Chem. 2006 Apr 6;49(7):2143-6. doi: 10.1021/jm051106d. J Med Chem. 2006. PMID: 16570908
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.
Das J, Furch JA, Liu C, Moquin RV, Lin J, Spergel SH, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Doweyko AM, Kamath A, Zhang H, Marathe P, Kanner SB, Lin TA, Dodd JH, Barrish JC, Wityak J. Das J, et al. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3706-12. doi: 10.1016/j.bmcl.2006.04.060. Epub 2006 May 6. Bioorg Med Chem Lett. 2006. PMID: 16682193
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
Borzilleri RM, Bhide RS, Barrish JC, D'Arienzo CJ, Derbin GM, Fargnoli J, Hunt JT, Jeyaseelan R Sr, Kamath A, Kukral DW, Marathe P, Mortillo S, Qian L, Tokarski JS, Wautlet BS, Zheng X, Lombardo LJ. Borzilleri RM, et al. J Med Chem. 2006 Jun 29;49(13):3766-9. doi: 10.1021/jm060347y. J Med Chem. 2006. PMID: 16789733
128 results