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

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 IC(50)...

Descripción completa

Detalles Bibliográficos
Autores principales: Li, Xingzhou, Zhou, Xinming, Zhang, Jing, Wang, Lili, Long, Long, Zheng, Zhibing, Li, Song, Zhong, Wu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271066/
https://www.ncbi.nlm.nih.gov/pubmed/24531217
http://dx.doi.org/10.3390/molecules19022004
Descripción
Sumario: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 IC(50) value of 0.033 μM, which is equipotent to that of BIRB796 (IC(50) = 0.032 μM).

Ejemplares similares