Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold

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 significa...

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Detalles Bibliográficos
Autores principales: Zhang, Wei, Ai, Jing, Shi, Dakuo, Peng, Xia, Ji, Yinchun, Liu, Jian, Geng, Meiyu, Li, Yingxia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271681/
https://www.ncbi.nlm.nih.gov/pubmed/24566328
http://dx.doi.org/10.3390/molecules19022655
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author Zhang, Wei
Ai, Jing
Shi, Dakuo
Peng, Xia
Ji, Yinchun
Liu, Jian
Geng, Meiyu
Li, Yingxia
author_facet Zhang, Wei
Ai, Jing
Shi, Dakuo
Peng, Xia
Ji, Yinchun
Liu, Jian
Geng, Meiyu
Li, Yingxia
author_sort Zhang, Wei
collection PubMed
description 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 IC(50) values of 8.6−81 nM and four compounds showed potent inhibitory activity against MKN45 cell proliferation, with IC(50)s ranging from 0.57−16 μM.
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spelling pubmed-62716812018-12-20 Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold Zhang, Wei Ai, Jing Shi, Dakuo Peng, Xia Ji, Yinchun Liu, Jian Geng, Meiyu Li, Yingxia Molecules Article 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 IC(50) values of 8.6−81 nM and four compounds showed potent inhibitory activity against MKN45 cell proliferation, with IC(50)s ranging from 0.57−16 μM. MDPI 2014-02-24 /pmc/articles/PMC6271681/ /pubmed/24566328 http://dx.doi.org/10.3390/molecules19022655 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Zhang, Wei
Ai, Jing
Shi, Dakuo
Peng, Xia
Ji, Yinchun
Liu, Jian
Geng, Meiyu
Li, Yingxia
Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold
title Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold
title_full Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold
title_fullStr Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold
title_full_unstemmed Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold
title_short Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold
title_sort discovery of novel c-met inhibitors bearing a 3-carboxyl piperidin-2-one scaffold
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271681/
https://www.ncbi.nlm.nih.gov/pubmed/24566328
http://dx.doi.org/10.3390/molecules19022655
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