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Synthesis of A New Class of Pyridazin-3-one and 2-Amino-5-arylazopyridine Derivatives and Their Utility in the Synthesis of Fused Azines
Molecules 2014, 19(2), 2655-2673; doi:10.3390/molecules19022655

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

1, 2, 3, 2, 2, 1, 2,*  and 1,*
1 School of Pharmacy, Fudan University, Shanghai 201203, China 2 Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China 3 School of Pharmacy, Ocean University of China, Qingdao 266003, China
* Authors to whom correspondence should be addressed.
Received: 21 January 2014 / Revised: 13 February 2014 / Accepted: 14 February 2014 / Published: 24 February 2014
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: c-Met; synthesis; kinase inhibitor; 3-carboxypiperidin-2-one c-Met; synthesis; kinase inhibitor; 3-carboxypiperidin-2-one
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Zhang, W.; Ai, J.; Shi, D.; Peng, X.; Ji, Y.; Liu, J.; Geng, M.; Li, Y. Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold. Molecules 2014, 19, 2655-2673.

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