研究简报

氮杂糖修饰的蒽醌衍生物的合成及细胞毒性

  • 张平竹 ,
  • 魏笑 ,
  • 刘欢 ,
  • 王齐伟 ,
  • 马趁 ,
  • 戎瑞雪 ,
  • 李小六
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  • 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

收稿日期: 2016-02-16

  修回日期: 2016-04-26

  网络出版日期: 2016-05-03

基金资助

国家自然科学基金(Nos. 21172051,21372059)资助项目.

Synthesis and Cytotoxicity of Azasugar Modified Anthraquinone Derivatives

  • Zhang Pingzhu ,
  • Wei Xiao ,
  • Liu Huan ,
  • Wang Qiwei ,
  • Ma Chen ,
  • Rong Ruixue ,
  • Li Xiaoliu
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  • Key Laboratory of Chemical Biology of Hebei Province, School of Chemistry and Environmental Science, Hebei University, Baoding 071002

Received date: 2016-02-16

  Revised date: 2016-04-26

  Online published: 2016-05-03

Supported by

Project supported by the National Natural Science Foundation of China (Nos. 21172051, 21372059).

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.

本文引用格式

张平竹 , 魏笑 , 刘欢 , 王齐伟 , 马趁 , 戎瑞雪 , 李小六 . 氮杂糖修饰的蒽醌衍生物的合成及细胞毒性[J]. 有机化学, 2016 , 36(8) : 1921 -1925 . DOI: 10.6023/cjoc201602012

Abstract

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 of N-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.

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