蒽醌-多胺缀合物的合成及生理活性研究  

Synthesis and Biological Activity of Anthraquinone-polyamine Derivatives

作　　者：甘莹[1] 何利华[1] 张亚宏[1] 王建红[1] 赵瑾[1] 

机构地区：[1]河南大学河南省天然药物与免疫工程重点实验室,开封475004

出　　处：《有机化学》2014年第3期589-595,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21272056);河南省科技厅(Nos.112300413224;132300410228)资助项目~~

摘　　要：设计合成7个蒽醌-多胺缀合物,化合物结构经1H NMR,APCI-MS和元素分析确认.利用MTT(噻唑蓝)法测试7个目标化合物对K562,HepG2,MB231,Hela,HCT-116五种肿瘤细胞的体外细胞毒性,结果表明所合成的化合物对测肿瘤细胞均具有明显的生长抑制作用.DNA结合实验表明11b和14c以嵌入方式作用于DNA,使鲱鱼精DNA-EB体系的荧光产生猝灭现象.Seven anthraquinone-polyamine derivatives were designed and synthesized. The structures of the synthesized compounds were confirmed by IH NMR, APCI-MS and elemental analysis. Prelimilary antitumor activity was invesitgated on K562, HepG2, MB231, Hela and HCT-116 cell lines by MTT （thiazolyl blue） assay. The results indicated that the target com- pounds obviously exhibited antitumor activity against the tested cell lines. Compounds 11b and 14c can intercalate to DNA with intensively fluorescence quenching in herring sperm DNA-EB system.

关 键 词：蒽醌衍生物 合成 生理活性 DNA嵌入剂 

分 类 号：TQ460.1[化学工程—制药化工]