N-(cycloalkylamino) acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1, 1-dimethylethyl)-2-oxazolyl] methyl] thio]-2-thiazolyl]-4- …

…, JT Hunt, DB Rawlins, W Shan, SZ Ahmed…

Index: Misra, Raj N.; Xiao, Hai-Yun; Kim, Kyoung S.; Lu, Songfeng; Han, Wen-Ching; Barbosa, Stephanie A.; Hunt, John T.; Rawlins, David B.; Shan, Weifang; Ahmed, Syed Z.; Qian, Ligang; Chen, Bang-Chi; Zhao, Rulin; Bednarz, Mark S.; Kellar, Kristen A.; Mulheron, Janet G.; Batorsky, Roberta; Roongta, Urvashi; Kamath, Amrita; Marathe, Punit; Ranadive, Sunanda A.; Sack, John S.; Tokarski, John S.; Pavletich, Nikola P.; Lee, Francis Y. F.; Webster, Kevin R.; Kimball, S. David Journal of Medicinal Chemistry, 2004 , vol. 47, # 7 p. 1719 - 1728

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Citation Number: 216

Abstract

N-Acyl-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. In particular, compound 21 {N-[5-[[[5-(1, 1-dimethylethyl)-2-oxazolyl] methyl] thio]-2-thiazolyl]- 4-piperidinecarboxamide, BMS-387032}, has been identified as an ATP-competitive and CDK2-selective inhibitor which has been selected to enter Phase 1 human clinical trials ...