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

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 inhi...

Descripción completa

Detalles Bibliográficos
Autores principales: Zhu, Dianxi, Li, Xingzhou, Zhong, Wu, Zhao, Dongmei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332430/
https://www.ncbi.nlm.nih.gov/pubmed/26378516
http://dx.doi.org/10.3390/molecules200916604
_version_ 1783387348903395328
author Zhu, Dianxi
Li, Xingzhou
Zhong, Wu
Zhao, Dongmei
author_facet Zhu, Dianxi
Li, Xingzhou
Zhong, Wu
Zhao, Dongmei
author_sort Zhu, Dianxi
collection PubMed
description 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.
format Online
Article
Text
id pubmed-6332430
institution National Center for Biotechnology Information
language English
publishDate 2015
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-63324302019-01-24 Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors Zhu, Dianxi Li, Xingzhou Zhong, Wu Zhao, Dongmei Molecules Article 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. MDPI 2015-09-11 /pmc/articles/PMC6332430/ /pubmed/26378516 http://dx.doi.org/10.3390/molecules200916604 Text en © 2015 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/4.0/).
spellingShingle Article
Zhu, Dianxi
Li, Xingzhou
Zhong, Wu
Zhao, Dongmei
Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors
title Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors
title_full Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors
title_fullStr Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors
title_full_unstemmed Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors
title_short Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors
title_sort design, synthesis and biological evaluation of novel substituted n,n′-diaryl ureas as potent p38 inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332430/
https://www.ncbi.nlm.nih.gov/pubmed/26378516
http://dx.doi.org/10.3390/molecules200916604
work_keys_str_mv AT zhudianxi designsynthesisandbiologicalevaluationofnovelsubstitutednndiarylureasaspotentp38inhibitors
AT lixingzhou designsynthesisandbiologicalevaluationofnovelsubstitutednndiarylureasaspotentp38inhibitors
AT zhongwu designsynthesisandbiologicalevaluationofnovelsubstitutednndiarylureasaspotentp38inhibitors
AT zhaodongmei designsynthesisandbiologicalevaluationofnovelsubstitutednndiarylureasaspotentp38inhibitors

Ejemplares similares