Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.
A series of novel 5-(benzyloxy)pyridin-2(1H)-ones were designed, synthesized and biologically evaluated for c-Met inhibition. Various amides and benzoimidazoles at C-3 position were investigated. A potent compound 12b with a c-Met IC50 of 12nM was identified. This compound exhibited potent inhibition of EBC-1 cell associated with c-Met constitutive activation and showed high selectivity for c-Met than other tested 11 kinases. The binding model 12b with c-Met was disclosed by docking analysis.
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GENE-Y GENE-Y CHEMICAL CHEMICAL CHEMICAL CHEMICAL GENE-Y GENE-Y GENE-Y GENE-Y GENE-N
c-Met c-Met amides benzoimidazoles 5-(benzyloxy)pyridin-2(1H)-ones 5-(benzyloxy)pyridin-2(1H)-one c-Met c-Met c-Met c-Met kinases