Synthesis and biological evaluation of new homocamptothecin analogs

被引：19
|
作者：
Luo, Yu [1 ]
Yu, Shanbao [1 ]
Tong, Linjiang [2 ]
Huang, Qingqing [1 ]
Lu, Wei [1 ]
Chen, Yi [2 ]
机构：
[1] E China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Inst Drug Discovery & Dev, Shanghai 200062, Peoples R China
[2] Chinese Acad Sci, SIBS, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 54卷
基金：
中国国家自然科学基金;
关键词：
Electron-withdrawing group; Homocamptothecin; Camptothecin; Anticancer drugs; RING-MODIFIED CAMPTOTHECIN; PLANT ANTITUMOR AGENTS; TOPOISOMERASE-I; LACTONE RING; CHEMICAL MODIFICATION; INHIBITORY-ACTIVITIES; ANTILEUKEMIC ACTIVITY; 7-ETHYLCAMPTOTHECIN; 20(S)-CAMPTOTHECIN; DERIVATIVES;
D O I：
10.1016/j.ejmech.2012.05.002
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In order to increase the stability of E-ring of homocamptothecins, the electron-withdrawing group -OH or -OAc was induced to alpha position of ring-E lactone. Ten new homocamptothecin analogs were synthesized. Most compounds showed potent in vitro anticancer activity and potent Topo I inhibition, which was equal or superior to that of CPT, SN-38 and 10-HCPT. The stability studies of this series also displayed significant improvement of the stability. (c) 2012 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：281 / 286
页数：6
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