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Molecules 2015, 20(9), 16604-16619; doi:10.3390/molecules200916604

Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors

1
Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China
2
Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China
*
Authors to whom correspondence should be addressed.
Academic Editor: James W. Leahy
Received: 26 August 2015 / Revised: 7 September 2015 / Accepted: 9 September 2015 / Published: 11 September 2015
(This article belongs to the Special Issue Kinase Inhibitor Chemistry)
View Full-Text   |   Download PDF [1255 KB, uploaded 11 September 2015]   |  

Abstract

A novel series of substituted N,N′-diaryl ureas that act as p38α inhibitors have been designed and synthesized based on two key residues (Gly110 and Thr106) that are different in p38α MAPK than in other kinases. Preliminary biological evaluation indicated that most compounds possessed good p38α inhibitory potencies. Among these compounds, 9g appeared to be the most powerful and is the main compound that we will study in the future. View Full-Text
Keywords: kinase inhibitor; p38 inhibitors; p38 MAPK; TNF-α; glycine flip kinase inhibitor; p38 inhibitors; p38 MAPK; TNF-α; glycine flip
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Zhu, D.; Li, X.; Zhong, W.; Zhao, D. Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors. Molecules 2015, 20, 16604-16619.

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