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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. Among authors: tokarski j. J Med Chem. 2004 Dec 30;47(27):6658-61. doi: 10.1021/jm049486a. J Med Chem. 2004. PMID: 15615512
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
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.
Misra RN, Rawlins DB, Xiao HY, Shan W, Bursuker I, Kellar KA, Mulheron JG, Sack JS, Tokarski JS, Kimball SD, Webster KR. Misra RN, et al. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1133-6. doi: 10.1016/s0960-894x(03)00034-9. Bioorg Med Chem Lett. 2003. PMID: 12643928
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.
Wrobleski ST, Chen P, Hynes J Jr, Lin S, Norris DJ, Pandit CR, Spergel S, Wu H, Tokarski JS, Chen X, Gillooly KM, Kiener PA, McIntyre KW, Patil-Koota V, Shuster DJ, Turk LA, Yang G, Leftheris K. Wrobleski ST, et al. Among authors: tokarski js. J Med Chem. 2003 May 22;46(11):2110-6. doi: 10.1021/jm020329q. J Med Chem. 2003. PMID: 12747783
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
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