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

ABSTRACT: We have identified a novel series of substituted N,N'-diarylurea p38? inhibitors. The inhibitory activity of the target compounds against the enzyme p38?, MAPKAPK2 in BHK cells, TNF-? release in LPS-stimulated THP-1 cells and p38? binding experiments were tested. Among these compounds, 25a inhibited the p38? enzyme with an IC50 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.

SUBMITTER: Zhu D

PROVIDER: S-EPMC6272846 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature

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

Zhu Dianxi D Xing Qifeng Q Cao Ruiyuan R Zhao Dongmei D Zhong Wu W

Molecules (Basel, Switzerland) 20160523 5

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 IC50 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. ...[more]

PMID: 27223276

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