Synthesis of 2-amino-4-(7-azaindol-3-yl) pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors

…, R Li, PJ Connolly, S Emanuel, SA Middleton

Index: Huang, Shenlin; Li, Ronghua; Connolly, Peter J.; Emanuel, Stuart; Middleton, Steven A. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 18 p. 4818 - 4821

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Citation Number: 25

Abstract

A novel series of 2-amino-4-(7-azaindol-3-yl) pyrimidines was discovered as cyclin dependent kinase 1 (CDK1) inhibitors. The core structure was synthesized via Pd (II) catalyzed coupling reaction. A number of analogues showed good potency for CDK1 and exhibited cellular antiproliferation activity. The structure–activity relationship is described.