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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 3.0).

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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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