Synthesis of a heterocyclic aza-enediyne and its DNA-cleavage properties

Authors
David, WM Kumar, D Kerwin, SM
Citation
Wm. David et al., Synthesis of a heterocyclic aza-enediyne and its DNA-cleavage properties, BIOORG MED, 10(22), 2000, pp. 2509-2512
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
22
Year of publication
2000
Pages
2509 - 2512
Database
ISI
SICI code
0960-894X(20001120)10:22<2509:SOAHAA>2.0.ZU;2-8
Abstract
The benzimidazolium salt 2, incorporating an aza-enediyne moiety, has been prepared and is shown to be a very effective DNA-cleavage agent under mild physiological conditions. Its mechanism of action is currently under invest igation but may involve the generation of a diradical intermediate, DNA alk ylation, or both. (C) 2000 Elsevier Science Ltd. All rights reserved.