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

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

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 v...

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Bibliographic Details
Main Authors: Xingzhou Li, Xinming Zhou, Jing Zhang, Lili Wang, Long Long, Zhibing Zheng, Song Li, Wu Zhong
Format: Article
Language:English
Published: MDPI AG 2014-02-01
Series:Molecules
Subjects:
kinase inhibitor
p38 MAPK
2H-chromenylurea
chromanyl-urea
Online Access:http://www.mdpi.com/1420-3049/19/2/2004
Description
Summary: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).
ISSN:1420-3049

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