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-resistant enterococci) within MIC range 0.5-8 microg/mL. According to the eukaryotic or prokaryotic data, 1a might be a first analogue to replace echinomycin.
Kim
Yun Bong
YB
Center for Molecular Design and Synthesis, Department of Chemistry, Korea Advanced Institute of Science and Technology, 305-701, Taejon, South Korea.
Kim
Yong Hae
YH
Park
Ju Youn
JY
Kim
Soo Kie
SK
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects / Q000502:physiology; D045744:Cell Line, Tumor; D004448:Echinomycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D011810:Quinoxalines; D004448:Echinomycin