Synthesis of phenanthroindolizidine alkaloids and evaluation of their antitumor activities and toxicities

被引:19
作者
Ikeda, Takashi [1 ]
Yaegashi, Takashi [1 ]
Matsuzaki, Takeshi [1 ]
Yamazaki, Ryuta [1 ]
Hashimoto, Syusuke [1 ]
Sawada, Seigo [1 ]
机构
[1] Yakult Cent Inst Microbiol Res, Kunitachi, Tokyo 1868650, Japan
关键词
Phenanthroindolizidine alkaloid; Antitumor activity; Toxicity; ANALOGS;
D O I
10.1016/j.bmcl.2011.07.120
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We previously reported that phenanthroindolizidine alkaloid 3 and its derivatives had markedly potent in vitro cytotoxicity. However, they had low in vivo antitumor activities and high in vivo toxicities, which was a serious problem. To address this problem, new phenanthroindolizidine derivatives were synthesized and their antitumor activities and toxicities were evaluated. This study describes the relationship between the chemical structures, antitumor activities, and toxicities of these phenanthroindolizidine derivatives. Based on its properties, compound 8 was found to be the most suitable potential antitumor agent. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5978 / 5981
页数:4
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