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.
Bibliographical noteFunding Information:
This work was supported by Grant No. R02-2002-000-00097-0 from Korea Science & Engineering Foundation.
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry