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Molecules 2016, 21(5), 612; doi:10.3390/molecules21050612

Discovery of Potent c-MET Inhibitors with New Scaffold Having Different Quinazoline, Pyridine and Tetrahydro-Pyridothienopyrimidine Headgroups

School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China
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Academic Editor: Derek J. McPhee
Received: 23 March 2016 / Revised: 4 May 2016 / Accepted: 5 May 2016 / Published: 11 May 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [5865 KB, uploaded 11 May 2016]   |  

Abstract

Cellular mesenchymal-epithelial transition factor (c-MET) is closely linked to human malignancies, which makes it an important target for treatment of cancer. In this study, a series of 3-methoxy-N-phenylbenzamide derivatives, N-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl) benzamide derivatives and N1-(3-fluoro-4-methoxyphenyl)-N3-(4-fluorophenyl) malonamide derivatives were designed and synthesized, some of them were identified as c-MET inhibitors. Among these compounds with new scaffolds having different quinazoline, pyridine and tetrahydro-pyridothienopyrimidine head groups, compound 11c, 11i, 13b, 13h exhibited both potent inhibitory activities against c-MET and high anticancer activity against tested cancer cell lines in vitro. In addition, kinase selectivity assay further demonstrated that both 13b and 13h are potent and selective c-MET inhibitors. Molecular docking supported that they bound well to c-MET and VEGFR2, which demonstrates that they are potential c-MET RTK inhibitors for cancer therapy. View Full-Text
Keywords: quinazoline; pyridine; tetrahydro-pyridothienopyrimidine; MET inhibitor; cancer therapy quinazoline; pyridine; tetrahydro-pyridothienopyrimidine; MET inhibitor; cancer therapy
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MDPI and ACS Style

Jiang, Y.; Zhang, K.; Gao, S.; Wang, G.; Huang, J.; Wang, J.; Chen, L. Discovery of Potent c-MET Inhibitors with New Scaffold Having Different Quinazoline, Pyridine and Tetrahydro-Pyridothienopyrimidine Headgroups. Molecules 2016, 21, 612.

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