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Molecules 2016, 21(5), 677; doi:10.3390/molecules21050677

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

1
Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, Liaoning, China
2
Laboratory of Computer-Aided Drug Design and Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Rd., Beijing 100850, China
*
Authors to whom correspondence should be addressed.
Academic Editor: James W. Leahy
Received: 11 April 2016 / Revised: 22 April 2016 / Accepted: 12 May 2016 / Published: 23 May 2016
(This article belongs to the Special Issue Kinase Inhibitor Chemistry)
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Abstract

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. View Full-Text
Keywords: P38 MAPK; BIRB-796; SPR; TNF-α P38 MAPK; BIRB-796; SPR; TNF-α
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Zhu, D.; Xing, Q.; Cao, R.; Zhao, D.; Zhong, W. Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N′-Diarylurea Derivatives. Molecules 2016, 21, 677.

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