Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: Protein structure-guided design and SAR

Christine M. Richardson,Douglas S. Williamson,Martin J. Parratt,Jenifer Borgognoni,Andrew D. Cansfield,Pawel Dokurno,Geraint L. Francis,Rob Howes,Jonathan D. Moore,James B. Murray,Alan Robertson,Allan E. Surgenor,Christopher J. Torrance

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3β (GSK-3β). One example had a CDK2 IC50 of 120nM and showed selectivity over GSK-3β of 167-fold.

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关键词

Structure-guided drug design,CDK2,Triazolo [1,5-a]pyrimidines,SAR,Potency,Selectivity

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