Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo [1, 2-b] pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor

S Huang, R Lin, Y Yu, Y Lu, PJ Connolly, G Chiu…

Index: Huang, Shenlin; Lin, Ronghui; Yu, Yang; Lu, Yanhua; Connolly, Peter J.; Chiu, George; Li, Shengjian; Emanuel, Stuart L.; Middleton, Steven A. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1243 - 1245

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Citation Number: 84

Abstract

The novel compound 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo [1, 2-b] pyridine was discovered to be a potent CDK1 inhibitor. Described here is the chemistry for its synthesis, including Pd (II) catalyzed Stille coupling reaction and sulfur (0) induced benzimidazole formation. Its effects on VEGFR-2 kinase activity and tumour cell proliferation are also described.