Synthesis and antitumor activity of heterocyclic acid ester derivatives of 20S-camptothecins  

作　　者：Di Zao Li Yan Li Xiao Guang Chen Chen Gen Zhu Jing Yang Hong Yan Liu Xian Dao Pan 

机构地区：[1]Institute of Materia Medica, Chinese Academy of Medical Sciences ＆ Peking Union Medical College, Beijing 100050, China

出　　处：《Chinese Chemical Letters》2007年第11期1335-1338,共4页中国化学快报（英文版）

摘　　要：A series of heterocyclic acid esters of camptothecins as new compounds had been synthesized by acylation method, their in vitro and in vivo antitumor activities were evaluated. The cytotoxic results showed that 6 possessed the best efficacy on six human cancer cell lines in the six classes of CPTs＇ derivatives. In vivo testing results indicated that 9 had better antitumor activity against mouse liver carcinoma H22 than topotecan.A series of heterocyclic acid esters of camptothecins as new compounds had been synthesized by acylation method, their in vitro and in vivo antitumor activities were evaluated. The cytotoxic results showed that 6 possessed the best efficacy on six human cancer cell lines in the six classes of CPTs＇ derivatives. In vivo testing results indicated that 9 had better antitumor activity against mouse liver carcinoma H22 than topotecan.

关 键 词：CAMPTOTHECIN SYNTHESIS Heterocyclic acid Antitumor activity 

分 类 号：R96[医药卫生—药理学]