182692-69-9Relevant articles and documents
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease
Helal, Christopher J.,Sanner, Mark A.,Cooper, Christopher B.,Gant, Thomas,Adam, Mavis,Lucas, John C.,Kang, Zhijun,Kupchinsky, Stanley,Ahlijanian, Michael K.,Tate, Bonnie,Menniti, Frank S.,Kelly, Kristin,Peterson, Marcia
, p. 5521 - 5525 (2007/10/03)
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 (IC50 = ca. 320 nM). 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.
