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Discovery of novel c-Met inhibitors bearing a 3-carboxyl piperidin-2-one scaffold.


ABSTRACT: A series of compounds containing a novel 3-carboxypiperidin-2-one scaffold based on the lead structure BMS-777607 were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against MKN45 cancer cell lines. The results indicated that five compounds exhibited significant inhibitory effect on c-Met with IC50 values of 8.6-81 nM and four compounds showed potent inhibitory activity against MKN45 cell proliferation, with IC50s ranging from 0.57-16 ?M.

SUBMITTER: Zhang W 

PROVIDER: S-EPMC6271681 | biostudies-literature | 2014 Feb

REPOSITORIES: biostudies-literature

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Discovery of novel c-Met inhibitors bearing a 3-carboxyl piperidin-2-one scaffold.

Zhang Wei W   Ai Jing J   Shi Dakuo D   Peng Xia X   Ji Yinchun Y   Liu Jian J   Geng Meiyu M   Li Yingxia Y  

Molecules (Basel, Switzerland) 20140224 2


A series of compounds containing a novel 3-carboxypiperidin-2-one scaffold based on the lead structure BMS-777607 were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against MKN45 cancer cell lines. The results indicated that five compounds exhibited significant inhibitory effect on c-Met with IC50 values of 8.6-81 nM and four compounds showed potent inhibitory activity against MKN45 cell proliferation, with IC50s ranging from 0.57-16 μM. ...[more]

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