title: Design, Synthesis and Biological Evaluation of Novel Substituted N,N'-Diaryl ureas as Potent p38 Inhibitors.
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.
authors.affiliation: Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. zhudianxi@126.com.
authors.forename: Dianxi
authors.initials: D
authors.lastname: Zhu
authors.affiliation: Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China. xingzhou1970@gmail.com.
authors.forename: Xingzhou
authors.initials: X
authors.lastname: Li
authors.affiliation: Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China. zhongwu@bmi.ac.cn.
authors.forename: Wu
authors.initials: W
authors.lastname: Zhong
authors.affiliation: Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. dongmeiz-67@163.com.
authors.forename: Dongmei
authors.initials: D
authors.lastname: Zhao
mesh_terms: D006801:Humans; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D014508:Urea / Q000737:chemistry*; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*
chemical_list: D047428:Protein Kinase Inhibitors; D014508:Urea; D048051:p38 Mitogen-Activated Protein Kinases
keywords: TNF-α; glycine flip; kinase inhibitor; p38 MAPK; p38 inhibitors