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 IC(50)...

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Autores principales: Li, Xingzhou, Zhou, Xinming, Zhang, Jing, Wang, Lili, Long, Long, Zheng, Zhibing, Li, Song, Zhong, Wu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271066/
https://www.ncbi.nlm.nih.gov/pubmed/24531217
http://dx.doi.org/10.3390/molecules19022004
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author Li, Xingzhou
Zhou, Xinming
Zhang, Jing
Wang, Lili
Long, Long
Zheng, Zhibing
Li, Song
Zhong, Wu
author_facet Li, Xingzhou
Zhou, Xinming
Zhang, Jing
Wang, Lili
Long, Long
Zheng, Zhibing
Li, Song
Zhong, Wu
author_sort Li, Xingzhou
collection PubMed
description 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 IC(50) value of 0.033 μM, which is equipotent to that of BIRB796 (IC(50) = 0.032 μM).
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spelling pubmed-62710662018-12-20 Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway Li, Xingzhou Zhou, Xinming Zhang, Jing Wang, Lili Long, Long Zheng, Zhibing Li, Song Zhong, Wu Molecules Article 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 IC(50) value of 0.033 μM, which is equipotent to that of BIRB796 (IC(50) = 0.032 μM). MDPI 2014-02-13 /pmc/articles/PMC6271066/ /pubmed/24531217 http://dx.doi.org/10.3390/molecules19022004 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Li, Xingzhou
Zhou, Xinming
Zhang, Jing
Wang, Lili
Long, Long
Zheng, Zhibing
Li, Song
Zhong, Wu
Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway
title Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway
title_full Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway
title_fullStr Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway
title_full_unstemmed Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway
title_short Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway
title_sort synthesis and biological evaluation of chromenylurea and chromanylurea derivatives as anti-tnf-α agents that target the p38 mapk pathway
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271066/
https://www.ncbi.nlm.nih.gov/pubmed/24531217
http://dx.doi.org/10.3390/molecules19022004
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