Substituted 4-(thiazol-5-yl)-2-(phenylamino) pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure–activity relationship, and …

…, M Noble, JA Endicott, C Pepper, S Wang

Index: Shao, Hao; Shi, Shenhua; Huang, Shiliang; Hole, Alison J.; Abbas, Abdullahi Y.; Baumli, Sonja; Liu, Xiangrui; Lam, Frankie; Foley, David W.; Fischer, Peter M.; Noble, Martin; Endicott, Jane A.; Pepper, Chris; Wang, Shudong Journal of Medicinal Chemistry, 2013 , vol. 56, # 3 p. 640 - 659

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Citation Number: 35

Abstract

Cancer cells often have a high demand for antiapoptotic proteins in order to resist programmed cell death. CDK9 inhibition selectively targets survival proteins and reinstates apoptosis in cancer cells. We designed a series of 4-thiazol-2-anilinopyrimidine derivatives with functional groups attached to the C5-position of the pyrimidine or to the C4-thiazol moiety and investigated their effects on CDK9 potency and selectivity. One of the most ...