| Literature DB >> 15482916 |
Christopher J Helal1, Mark A Sanner, Christopher B Cooper, Thomas Gant, Mavis Adam, John C Lucas, Zhijun Kang, Stanley Kupchinsky, Michael K Ahlijanian, Bonnie Tate, Frank S Menniti, Kristin Kelly, Marcia Peterson.
Abstract
High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide (1). This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC(50)=ca. 320nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved.Entities:
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Year: 2004 PMID： 15482916 DOI： 10.1016/j.bmcl.2004.09.006
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823