Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives

We have identified a novel series of substituted N,N′-diarylurea p38α inhibitors. The inhibitory activity of the target compounds against the enzyme p38α, MAPKAPK2 in BHK cells, TNF-α release in LPS-stimulated THP-1 cells and p38α binding experiments were tested. Among these compounds, 25a inhibited...

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Autores principales: Zhu, Dianxi, Xing, Qifeng, Cao, Ruiyuan, Zhao, Dongmei, Zhong, Wu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272846/
https://www.ncbi.nlm.nih.gov/pubmed/27223276
http://dx.doi.org/10.3390/molecules21050677
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author Zhu, Dianxi
Xing, Qifeng
Cao, Ruiyuan
Zhao, Dongmei
Zhong, Wu
author_facet Zhu, Dianxi
Xing, Qifeng
Cao, Ruiyuan
Zhao, Dongmei
Zhong, Wu
author_sort Zhu, Dianxi
collection PubMed
description We have identified a novel series of substituted N,N′-diarylurea p38α inhibitors. The inhibitory activity of the target compounds against the enzyme p38α, MAPKAPK2 in BHK cells, TNF-α release in LPS-stimulated THP-1 cells and p38α binding experiments were tested. Among these compounds, 25a inhibited the p38α enzyme with an IC(50) value of 0.47 nM and a KD value of 1.54 × 10(−8) and appears to be the most promising one in the series.
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spelling pubmed-62728462018-12-28 Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives Zhu, Dianxi Xing, Qifeng Cao, Ruiyuan Zhao, Dongmei Zhong, Wu Molecules Article We have identified a novel series of substituted N,N′-diarylurea p38α inhibitors. The inhibitory activity of the target compounds against the enzyme p38α, MAPKAPK2 in BHK cells, TNF-α release in LPS-stimulated THP-1 cells and p38α binding experiments were tested. Among these compounds, 25a inhibited the p38α enzyme with an IC(50) value of 0.47 nM and a KD value of 1.54 × 10(−8) and appears to be the most promising one in the series. MDPI 2016-05-23 /pmc/articles/PMC6272846/ /pubmed/27223276 http://dx.doi.org/10.3390/molecules21050677 Text en © 2016 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 (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Zhu, Dianxi
Xing, Qifeng
Cao, Ruiyuan
Zhao, Dongmei
Zhong, Wu
Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives
title Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives
title_full Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives
title_fullStr Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives
title_full_unstemmed Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives
title_short Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives
title_sort synthesis and p38 inhibitory activity of some novel substituted n,n′-diarylurea derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272846/
https://www.ncbi.nlm.nih.gov/pubmed/27223276
http://dx.doi.org/10.3390/molecules21050677
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AT xingqifeng synthesisandp38inhibitoryactivityofsomenovelsubstitutednndiarylureaderivatives
AT caoruiyuan synthesisandp38inhibitoryactivityofsomenovelsubstitutednndiarylureaderivatives
AT zhaodongmei synthesisandp38inhibitoryactivityofsomenovelsubstitutednndiarylureaderivatives
AT zhongwu synthesisandp38inhibitoryactivityofsomenovelsubstitutednndiarylureaderivatives

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