Synthesis and biological evaluation of new homocamptothecin analogs

被引：18

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

页码：281 / 286

页数：6

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