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Synthesis and biological activity of new quinoxaline antibiotics of echinomycin analogues

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 1a shows remarkable cytotoxicities against human tumor various cell lines, and is active VRE (vancomycin-resistan...

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Published in:Bioorganic & medicinal chemistry letters 2004-01, Vol.14 (2), p.541-544
Main Authors: Kim, Yun Bong, Kim, Yong Hae, Park, Ju Youn, Kim, Soo Kie
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Language:English
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description 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 1a shows remarkable cytotoxicities against human tumor various cell lines, and is active VRE (vancomycin-resistant enterococci) within MIC range 0.5–8 μg/mL. According to the eukaryotic or prokaryotic data, 1a might be a first analogue to replace echinomycin. The novel compound 1a shows potential activities against various human cancer cell lines.
doi_str_mv 10.1016/j.bmcl.2003.09.086
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ispartof Bioorganic & medicinal chemistry letters, 2004-01, Vol.14 (2), p.541-544
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subjects Active-VRE
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Anticancer
Apoptosis
Apoptosis - drug effects
Apoptosis - physiology
Biological and medical sciences
Cell Line, Tumor
Echinomycin
Echinomycin - analogs & derivatives
Echinomycin - chemical synthesis
Echinomycin - pharmacology
Humans
Medical sciences
Miscellaneous. Antibiotics with multiple activities
Pharmacology. Drug treatments
Quinoxalines - chemical synthesis
Quinoxalines - pharmacology
title Synthesis and biological activity of new quinoxaline antibiotics of echinomycin analogues
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