Design, synthesis and anti-proliferative effects in tumor cells of new combretastatin A-4 analogs

作     者：Lei Zhao Jiu-Jiu Zhou Xin-Ying Huang Li-Ping Cheng Wan Pang Zhen-Peng Kai Fan-Hong Wu 

作者机构：School of Chemical and Environmental Engineering Shanghai Institute of Technology 

基　　金：supported by the National Natural Science Foundation of China(Nos.21472126,21402122) Shanghai Municipal Natural Science Foundation(No.12ZR450200) 

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

年 卷 期：2015年第26卷第8期

页      码：993-999页

摘      要：A total of 11 novel combretastatin A-4（CA-4） analogs were designed, synthesized, and evaluated for the anti-proliferative effects in tumor cells. The compounds represent four structural classes：（i）hydrogenated derivatives,（ii） ethoxyl derivatives,（iii） amino derivatives and（iv） pro-drugs. Biological evaluations demonstrate that multiple structural features control the biological potency. Three of the compounds, sit-1, sit-2 and sit-3, have potent anti-proliferative activity against multiple cancer cell lines. Their pro-drugs were synthesized to increase water solubility. Structure–activity relationship study and Surflex-Docking were studied in this paper. These results will be useful for the design of new CA-4 analogs that are structurally related to the SAR study.

主 题 词：analogs proliferative potent structurally completion afford Fmoc solubility cytotoxicity dissolved 

学科分类：1007[医学-药学类] 10[医学] 

核心收录：

D　O　I：10.1016/j.cclet.2015.05.003

馆 藏 号：203307686...