A novel class of cyclophosphamide prodrug:structure-activity relationships of cyclophosphamide piperaziniums

作     者：杨青 朱继让 孙崎 崔景荣 李润涛 葛泽梅 

作者机构：北京大学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 

基　　金：Foundation items:National Nature Science Foundation of China (Grant No. 20472008) the Major State Basic Research Development Program (Grant No. 2004CB719900) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2010年第19卷第1期

页      码：24-33页

摘      要：A new strategy for the modification of cyclophosphamide was carried out and three series of new cyclophosphamide piperazinium salts 10,11 and 13 were *** compounds,based on compound 9i scaffold,were evaluated for their in vivo anticancer activities against hepatocyte sarcoma 22 （H 22）.The structure-activity relationship study reveals that 1） the conformation and the substituent at N-3 of cyclophosphamide spiropiperazinium salts 10 greatly affect the activity 2） different kinds of cyclophosphamide non-spiropiperazinium derivatives 11 show different activities 3） for 1,2-benzisoxazole phosphoropiperazinium salts 13,it is possible to obtain anticancer drug candidates with suitable quaternary ammonium *** results would help to further design and synthesize analogs of mustard anticancer drugs.

主 题 词：Cyclophosphamide piperaziniums Prodrug Anticancer activity Synthesis DNA binding 

学科分类：1007[医学-药学类] 100701[100701] 10[医学] 

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