Title of article :
Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor
Author/Authors :
Shenlin Huang، نويسنده , , Ronghui Lin، نويسنده , , Yang Yu، نويسنده , , Yanhua Lu، نويسنده , , Peter J. Connolly، نويسنده , , George Chiu، نويسنده , , Shengjian Li، نويسنده , , Stuart L. Emanuel، نويسنده , , Steven A. Middleton، نويسنده ,
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.