Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor |
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| Authors: | Huang Shenlin Lin Ronghui Yu Yang Lu Yanhua Connolly Peter J Chiu George Li Shengjian Emanuel Stuart L Middleton Steven A |
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| Affiliation: | Johnson & Johnson Pharmaceutical Research & Development L. L. C., 1000 Route 202, Raritan, NJ 08869, USA. shenlinhuang@hotmail.com |
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| 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. |
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