Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and x-ray crystallographic analysis

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. A novel series of anilinopyrazoles...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-09, Vol.13 (18), p.2985-2988
Hauptverfasser:	Tang, Jun, Shewchuk, Lisa M., Sato, Hideyuki, Hasegawa, Masaichi, Washio, Yoshiaki, Nishigaki, Naohiko
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites CDC2-CDC28 Kinases - antagonists & inhibitors CDC2-CDC28 Kinases - chemistry Crystallography, X-Ray Cyclin-Dependent Kinase 2 Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Humans Inhibitory Concentration 50 Models, Molecular Protein Binding Pyrazoles - chemical synthesis Pyrazoles - pharmacology Structure-Activity Relationship
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Zusammenfassung:	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. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00630-9