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。
基金
National Natural Science Foundation of China (Grant No.20472008)
Fund for Young Teachers of School of Pharmaceutical Sciences,Peking University
