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Synthesis and biological evaluation of Chromenylurea and Chromanylurea derivatives as anti-TNF-? agents that target the p38 MAPK pathway.

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-? production in lipopolysaccharide-stimulated THP-1 cells. The most active compound, 40g, inhibited TNF-? release with an IC50 value of 0.033 ?M, which is equipotent to that of BIRB796 (IC50 = 0.032 ?M).

SUBMITTER: Li X

PROVIDER: S-EPMC6271066 | biostudies-literature | 2014 Feb

REPOSITORIES: biostudies-literature

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Synthesis and biological evaluation of Chromenylurea and Chromanylurea derivatives as anti-TNF-α agents that target the p38 MAPK pathway.

Li Xingzhou X Zhou Xinming X Zhang Jing J Wang Lili L Long Long L Zheng Zhibing Z Li Song S Zhong Wu W

Molecules (Basel, Switzerland) 20140213 2

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). ...[more]

PMID: 24531217

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