Modification of the alkylating agent chlorambucil with spiropiperazinium salts  

螺环季铵盐修饰的苯丁酸氮芥类抗肿瘤化合物(英文)

作　　者：李功[1] 孙崎 崔景荣 李润涛 

机构地区：[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

出　　处：《Journal of Chinese Pharmaceutical Sciences》2010年第5期346-352,共7页中国药学（英文版）

基　　金：National Natural Science Foundation of China (Grant No.20472008);Fund for Young Teachers of School of Pharmaceutical Sciences,Peking University

摘　　要：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.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H_(22)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：CHLORAMBUCIL Antitumor activity Spiropiperazinium SAR 

分 类 号：R96[医药卫生—药理学]