氮杂糖修饰的蒽醌衍生物的合成及细胞毒性  

Synthesis and Cytotoxicity of Azasugar Modified Anthraquinone Derivatives

作　　者：张平竹[1] 魏笑[1] 刘欢[1] 王齐伟[1] 马趁 戎瑞雪[1] 李小六[1] 

机构地区：[1]河北大学化学与环境科学学院河北省化学生物学重点实验室,保定071002

出　　处：《有机化学》2016年第8期1921-1925,共5页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.21172051;21372059)资助项目~~

摘　　要：为开发低毒、高效的蒽醌类抗肿瘤化合物,设计并利用N-烷氨基氮杂糖与大黄酸的缩合反应,及N-烷氨基氮杂糖与1-氨基-4-溴蒽酮-2-磺酸的微波促进Cu0催化乌尔曼偶联(Ullmann coupling)反应,合成系列新型氮杂糖修饰的蒽醌衍生物.对所合成的化合物进行了初步体外肿瘤细胞(Hela、A549、MCF-7和MGC-803)的细胞毒性测试.In order to develop the anti-tumor agents with high efficiency and low toxicity, a series of novel azasugar modified anthraquinone derivatives have been designed and synthesized by the ammonolysis of N-alkylamino azasugar with rhine and microwave assisted Ullmann coupling reaction ofN-alkylamino azasugar with 1-amino-4-bromoanthraquinone-2-sulfonic acid. Their cytotoxic activities against Hela, A549, MCF-7 and MGC-803 cells were preliminarily evaluated.

关 键 词：蒽醌 大黄酸 氮杂糖 乌尔曼偶联 细胞毒性 

分 类 号：O625.463[理学—有机化学]