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Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic
Jun Tang1, Lisa M Shewchuk, Hideyuki Sato
1GlaxoSmithKline K. K. Tsukuba Research Laboratories, 43 Wadai Tsukuba, Ibaraki 300-4247, Japan. jt21064@gsk.com
Bioorganic & Medicinal Chemistry Letters
|August 28, 2003
Abstract:
A novel series of anilinopyrazoles has been designed based on the X-ray crystal structure analysis. Most compounds from this series not only show sub-nanomolar IC(50) values for CDK2, but also demonstrate almost 1000-fold selectivity to other kinases including CDK1.