Synthesis of a heterocyclic aza-enediyne and its DNA-cleavage properties.
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 investigation but may involve the generation of a diradical intermediate. DNA alkylation, or both.
David
W M
WM
Division of Medicinal Chemistry, College ot Pharmacy and Institute for Cellular and Molecular Biology, University of Texas at Austin, 78712, USA.
Kumar
D
D
Kerwin
S M
SM
D001372:Aza Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D004247:DNA / Q000737:chemistry / Q000187:drug effects*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology
D001372:Aza Compounds; D006571:Heterocyclic Compounds; D004247:DNA