Design, synthesis and in vitro antitumor evaluation of novel diaryl urea derivatives bearing sulfonamide moiety

作     者：LUO Can TANG Ke LI Yan YIN DaLi CHEN XiaoGuang HUANG HaiHong 

作者机构：Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation Institute of Materia MedicaPeking Union Medical College & Chinese Academy of Medical Sciences 

基　　金：financially supported by the National Science&Technology Major Project(2009ZX09301-003-9-1) 

出 版 物：《Science China Chemistry》 (中国科学（化学英文版）)

年 卷 期：2013年第56卷第11期

页      码：1564-1572页

摘      要：A novel series of diaryl urea derivatives bearing sulfonamide moiety have been designed and synthesized. Their in vitro antitumor effect against human cancer cell lines MX-1, A375, HepG2, Ketr3 and HT-29 was screened and evaluated by the standard MTT assay with sorafenib as the positive control. Some of the compounds showed significant inhibitory activity against multiple cell lines compared to sorafenib. In particular, 2,6-dimethyl-4-{6-[3-（4-chloro-3-（trifluoromethyl）phenyl）urealnaphthalen- 2-yllsulfonyl morpholine （10d） was found to be the most potent against A375, HepG2 and Ketr3 with ICs0 values of 0.65-0.97 μmol/L, which were 5-20-fold more potent than sorafenib. Compound 10d emerged as a valuable lead for further optimization.

主 题 词：diaryl urea derivatives sulfonamide sorafenib antitumor activity 

学科分类：1007[医学-药学类] 0703[理学-化学类] 10[医学] 

核心收录：

D　O　I：10.1007/s11426-013-4903-z

馆 藏 号：203227384...