DNA-cleavage studies on N-substituted monocyclic enediynes: Enhancement ofpotency by incorporation of intercalating or electron poor aromatic ring and subsequent design of a novel phototriggerable acyclic enediyne

Citation
A. Basak et al., DNA-cleavage studies on N-substituted monocyclic enediynes: Enhancement ofpotency by incorporation of intercalating or electron poor aromatic ring and subsequent design of a novel phototriggerable acyclic enediyne, BIOORG MED, 10(12), 2000, pp. 1321-1325
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
12
Year of publication
2000
Pages
1321 - 1325
Database
ISI
SICI code
0960-894X(20000619)10:12<1321:DSONME>2.0.ZU;2-Y
Abstract
A number of novel N-substituted enediynes (azaenediynes) 1-4 were synthesiz ed as DNA cleaving agents. Enhancement of DNA cleavage potency was observed with those compounds which could interact with DNA through intercalation o f the extended aromatic ring or through electrostatic attraction with elect ron poor aromatic ring. An acyclic enediyne 5 with a novel phototriggerable device was also synthesized and its DNA-cleaving activity was established. (C) 2000 Elsevier Science Ltd. All rights reserved.