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Molecules. 2014 Feb 24;19(2):2655-73. doi: 10.3390/molecules19022655.

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

Author information

  • 1School of Pharmacy, Fudan University, Shanghai 201203, China.
  • 2Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
  • 3School of Pharmacy, Ocean University of China, Qingdao 266003, China.
  • 4Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. mygeng@simm.ac.cn.
  • 5School of Pharmacy, Fudan University, Shanghai 201203, China. liyx417@fudan.edu.cn.

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 μM.

PMID:
24566328
[PubMed - in process]
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