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...

Full description

Saved in:
Bibliographic Details
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
Format: Article
Language:English
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
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.09.086