Synthesis and biological activity of new quinoxaline antibiotics of echinomycin analogues

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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.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Issue Date
2004
Language
English
Article Type
Article
Keywords

DES-N-TETRAMETHYLTRIOSTIN; THIOL PROTECTING GROUP; TRIOSTIN-A; DERIVATIVES; ACID; CYSTEINE; CYSTINE; BINDING

Citation

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.14, no.2, pp.541 - 544

ISSN
0960-894X
DOI
10.1016/j.bmcl.2003.09.086
URI
http://hdl.handle.net/10203/80894
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