Synthesis and biological activity of new quinoxaline antibiotics of echinomycin analogues

被引:288
|
作者
Kim, YB
Kim, YH [1 ]
Park, JY
Kim, SK
机构
[1] Korea Adv Inst Sci & Technol, Ctr Mol Design & Synth, Dept Chem, Taejon 305701, South Korea
[2] Yonsei Univ, Dept Microbiol, Wonju Coll Med, Inst Basic Med Sci,IFBB, Wonju 220701, South Korea
关键词
echinomycin; anticancer; active-VRE; apoptosis;
D O I
10.1016/j.bmcl.2003.09.086
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Novel quinoxaline antibiotics having the methylenedithioether bridge as an analogue of echinomycin have been synthesized by insertion of methylene moiety between -S-S- bond. The compound la shows remarkable cytotoxicities against human tumor various cell lines, and is active VRE (vancomycin-resistant enterococci) within MIC range 0.5-8 mug/mL. According to the eukaryotic or prokaryotic data, la might be a first analogue to replace echinomycin. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:541 / 544
页数:4
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