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Molecules 2014, 19(2), 2004-2028; doi:10.3390/molecules19022004
Article

Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway

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Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China These authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 17 December 2013 / Revised: 28 January 2014 / Accepted: 28 January 2014 / Published: 13 February 2014
(This article belongs to the Section Medicinal Chemistry)
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Abstract

A series of 1-aryl-3-(2H-chromen-5-yl)urea and 1-aryl-3-(chroman-5-yl)urea derivatives were designed, synthesized and evaluated for their inhibitory activities towards TNF-α production in lipopolysaccharide-stimulated THP-1 cells. The most active compound, 40g, inhibited TNF-α release with an IC50 value of 0.033 μM, which is equipotent to that of BIRB796 (IC50 = 0.032 μM).
Keywords: kinase inhibitor; p38 MAPK; 2H-chromenylurea; chromanyl-urea kinase inhibitor; p38 MAPK; 2H-chromenylurea; chromanyl-urea
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Li, X.; Zhou, X.; Zhang, J.; Wang, L.; Long, L.; Zheng, Z.; Li, S.; Zhong, W. Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway. Molecules 2014, 19, 2004-2028.

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