Add time:07/29/2019         Source:sciencedirect.com

c-Met was emerging as an attractive target for cancer-targeted therapy because deregulation of c-Met has been observed in multiple tumor types. A series of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives were designed, synthesized and evaluated for their enzymatic inhibitory activity against c-Met kinase and cellular potency against MKN45, EBC-1 and PC-3 cell lines. Nine of them showed better activity than lead compound 1 which was found via computer-aided drug design. Among them, compound 8c showed inhibitory activity of 68 nM against c-Met and low micromole cellular potency against MKN45 and EBC-1 cell lines. Moreover, 8c demonstrated more than 50-fold selectivity against other tyrosine kinases tested. The result of western blot indicated that compound 8c was capable of inhibiting the phosphorylation of c-Met kinase in MKN45 cell line in a dose-dependent manner.

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