Anticancer activity and DNA binding property of the trimers of triphenylethylene-coumarin hybrids

作     者：Li Zhang Yu-Chao Yao Meng-Ying Gao Rui-Xue Rong Ke-Rang Wang Xiao-Liu Li Hua Chen 

作者机构：Key Laboratory of Chemical Biology of Hebei ProvinceCollege of Chemistry and Environmental ScienceHebei University 

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

年 卷 期：2016年第27卷第11期

页      面：1708-1716页

核心收录：

学科分类：1008[医学-中药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

基　　金：the National Natural Science Foundation of China(NSFC No.20902016) 

主　　题：Coumarin Triphenylethylene TrimerAnti tumor activity DNA binding property 

摘      要：Novel trimers of triphenylethylene-coumarin hybrid containing two amino side chains （5a-d and 6a-d） were designed and synthesized by the condensation of 1,3,5-benzenetricarboxylic acid with the varied amino monomeric hybrids catalyzed by HATU and DIPEA at room temperature. The extended trimeric compound 6a （R = piperidinyl） exhibited significant anti-proliferative activity against three cancer cells at IC5o of near 10 μmol/L. UV-vis, fluorescence （lifetime） and thermal denaturation exhibited that 6a had significant interaction with Ct-DNA by the intercalative mode of binding. The order of their anti- proliferative activities was 6（a, d） 〉 5（a, d） and （5-6）a 〉 （5-6）d, respectively, in accordance with that of their DNA binding properties, which suggested that the prolonged linker （six carbons） and piperidinyl ~roun on the side chains are beneficial to DNA binding and the anti-tumor activity.