Synthesis and Biological Evaluation of Chromenylurea and Chromanylurea Derivatives as Anti-TNF-α agents that Target the p38 MAPK Pathway

Molecules

Xingzhou Li¹  Xinming Zhou¹  Jing Zhang²  Lili Wang²  Long Long²  Zhibing Zheng²  Song Li² 

[1] Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China;

关键词: kinase inhibitor;    p38 MAPK;    2H-chromenylurea;    chromanyl-urea;   

DOI  :  10.3390/molecules19022004

来源: mdpi

【 摘 要 】

A series of 1-aryl-3-(2H-chromen-5-yl)urea and 1-aryl-3-(chroman-5-yl)urea derivatives were designed, synthesized and evaluated for their inhibitory activities towards TNF-α production in lipopolysaccharide-stimulated THP-1 cells. The most active compound, 40g, inhibited TNF-α release with an IC₅₀ value of 0.033 μM, which is equipotent to that of BIRB796 (IC₅₀ = 0.032 μM).

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.