有机化学 ›› 2016, Vol. 36 ›› Issue (8): 1921-1925.DOI: 10.6023/cjoc201602012 上一篇    下一篇

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   

  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
  • 收稿日期:2016-02-16 修回日期:2016-04-26 发布日期:2016-05-03
  • 通讯作者: 李小六 E-mail:lixl@hbu.cn
  • 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   

  1. Key Laboratory of Chemical Biology of Hebei Province, School of Chemistry and Environmental Science, Hebei University, Baoding 071002
  • Received:2016-02-16 Revised:2016-04-26 Published:2016-05-03
  • Supported by:

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

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.

关键词: 蒽醌, 大黄酸, 氮杂糖, 乌尔曼偶联, 细胞毒性

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.

Key words: anthraquinone, rhein, azasugar, Ullmann coupling, cytotoxicity