| Literature DB >> 15125971 |
Raj N Misra1, Hai-yun Xiao, David K Williams, Kyoung S Kim, Songfeng Lu, Kristen A Keller, Janet G Mulheron, Roberta Batorsky, John S Tokarski, John S Sack, S David Kimball, Francis Y Lee, Kevin R Webster.
Abstract
N-Aryl aminothiazoles 6-9 were prepared from 2-bromothiazole 5 and found to be CDK inhibitors. In cells they act as potent cytotoxic agents. Selectivity for CDK1, CDK2, and CDK4 was dependent of the nature of the N-aryl group and distinct from the CDK2 selective N-acyl analogues. The N-2-pyridyl analogues 7 and 19 showed pan CDK inhibitory activity. Elaborated analogues 19 and 23 exhibited anticancer activity in mice against P388 murine leukemia. The solid-state structure of 7 bound to CDK2 shows a similar binding mode to the N-acyl analogues.Entities:
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Year: 2004 PMID： 15125971 DOI： 10.1016/j.bmcl.2004.02.105
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823