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Synthesis and biological activity of new quinoxaline antibiotics of echinomycin analogues

2003; Elsevier BV; Volume: 14; Issue: 2 Linguagem: Inglês

10.1016/j.bmcl.2003.09.086

1464-3405

Yun Bong Kim, Yong Hae Kim, Ju Youn Park, Soo Kie Kim,

Synthesis and Reactions of Organic Compounds

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.