Synthesis and cytotoxic activities of E-resveratrol derivatives

作     者：HONG Ting JIANG Wei DONG Huai-Ming QIU Sheng-Xiang LU Yu 

作者机构：Sino-German Joint Research Institute of Nanchang University Jiangxi Provincial Institute for Food and Drug ControlJiangxi Provincial Engineering Research Center for Drug and Medical Device Quality Chinese Academy of SciencesSouth China Botanical Garden 

出 版 物：《Chinese Journal of Natural Medicines》 (中国天然药物（英文版）)

年 卷 期：2015年第13卷第5期

页      面：375-382页

核心收录：

学科分类：0710[理学-生物学] 1008[医学-中药学(可授医学、理学学位)] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 1005[医学-中医学] 100706[医学-药理学] 1002[医学-临床医学] 0703[理学-化学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：supported by the Cross-fund of Nanchang University 

主　　题：E-resveratrol derivatives Synthesis Cytotoxic activity Structure–activity relationships 

摘      要：The present study was designed to synthesize derivatives of E-resveratrol and evaluate their cytotoxic activity in *** functional groups were conjugated with the phenolic hydroxyl group of E-resveratrol,and the double bond of E-resveratrol was *** in vitro cytotoxicity of the synthetic derivatives was evaluated against three tumor cell lines(A549,LAC,and He La) using the MTT ***-six E-resveratrol derivatives were synthesized and their structures were confirmed by 1H NMR,MS,IR,and elemental *** 1-6,12,15-21,and 23-26 were reported for the first *** them,Compounds 1,2,4,5,and 9-11,showed significant cytotoxicity against tumor cells;especially,Compound 1 showed an IC50 value of 4.38 μmol·L-1 in the A549 cells which was 15-fold more active than E-resveratrol;Compound 9 showed an IC50 value of 1.41 μmol·L-1 in the He La cell line which was 90-fold more active than E-resveratrol,and close to *** structure–activity relationships were also *** 1,2 and 9-11 may serve as potential lead compounds for the discovery of new anticancer drugs.