http://jcps.bjmu.edu.cn

• 研究论文 • 上一篇    下一篇

螺环季铵盐修饰的苯丁酸氮芥类抗肿瘤化合物

李功, 孙崎*, 崔景荣, 李润涛*   

  1. 北京大学医学部 天然药物及仿生药物国家重点实验室; 药学院 化学生物学系, 北京 100191
  • 收稿日期:2010-06-28 修回日期:2010-08-12 出版日期:2010-09-20 发布日期:2010-09-20
  • 通讯作者: 孙崎*, 李润涛*

Modification of the alkylating agent chlorambucil with spiropiperazinium salts

Gong Li, Qi Sun*, Jing-Rong Cui, Run-Tao Li*   

  1. State Key Laboratory of Natural and Biomimetic drugs; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2010-06-28 Revised:2010-08-12 Online:2010-09-20 Published:2010-09-20
  • Contact: Qi Sun*, Run-Tao Li*

摘要: 本文合成了一系列苯丁酸氮芥季铵盐类抗肿瘤化合物8a-8f, 并对其抗肿瘤活性进行了初步测试。结果显示: 化合物8f 的体内抗H22活性最强, 优于阳性对照药苯丁酸氮芥。文中所揭示的构效关系, 对进一步结构优化具有一定的指导意义。

关键词: 苯丁酸氮芥, 抗肿瘤活性, 螺环季铵盐, SAR

Abstract: In order to improve the antitumor activity and reduce the toxicity of the alkylating agent chlorambucil, a series of spiropiperazinium salts of chlorambucil (8) were designed and synthesized. It was found that compound 8f exhibited potential in vivo activity against H22.

Key words: Chlorambucil, Antitumor activity, Spiropiperazinium, SAR

中图分类号: 

Supporting:

Foundation items: National Natural Science Foundation of China (Grant No. 20472008) and Fund for Young Teachers of School of Pharmaceutical Sciences, Peking University.
*Corresponding author. Tel.: 86-10-82801504