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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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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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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