Molecules

Synthesis and biological evaluation of chromenylurea and chromanylurea derivatives as anti-TNF-α agents that target the p38 MAPK pathway

X Li, X Zhou, J Zhang, L Wang, L Long, Z Zheng, S Li…

Index: Li, Xingzhou; Zhou, Xinming; Zhang, Jing; Wang, Lili; Long, Long; Zheng, Zhibing; Li, Song; Zhong, Wu Molecules, 2014 , vol. 19, # 2 p. 2004 - 2028

Full Text: HTML

Citation Number: 6

Abstract

Abstract: A series of 1-aryl-3-(2 H-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).