Synthesis and biological evaluation of 5,6,7-trimethoxy-1-benzylidene-3,4-dihydro-naphthalen-2-one as tubulin-polymerization inhibitors

作     者：Jun-Hang Jiang Can-Hui Zheng Chong-Qing Wang Juan Wang Wei Tian Chao Yang Yun-Long Song Yong Hu Ju Zhu You-Yun Zhou 

作者机构：School of PharmacySecond Military Medical University Shanghai Institute of Pharmaceutical Industry Department of NeonatologyShanghai Children's HospitalShanghai Jiao Tong University 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2015年第26卷第5期

页      面：607-609页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 0703[理学-化学] 10[医学] 

基　　金：supported by the National Natural Science Foundation of China(Nos.21172260 and 30901859) Shanghai Natural Science Foundation(No.09ZR1438800) "Chen Guang" Project supported by Shanghai Municipal Education Commission and Shanghai Education Development Foundation(No.12CG42) 

主　　题：Tubulin polymerization inhibitor Antitumor agent Combretastatin A4 analog 

摘      要：A series of new combretastatin-A4 analogs were synthesized, in which a six-membered ring connects the linking bridge and A ring, and their tumor cell growth and tubulin-polymerization inhibitory activity were evaluated. These compounds appear to be potential tubulin-polymerization inhibitors, Compounds 1b with amino substituted on position 3 of B ring conferred optimal bioactivity, higher than that of the lead compound 22b and equivalent to that of CA-4. The binding modes of these compounds to tuhulin were obtained by molecular docking, which can explain the structure-activity relationship. The studies presented here provide a new structural type for the development of novel antitumor agents.