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

A number of novel N-substituted enediynes (azaenediynes) 1– 4 were synthesized as DNA cleaving agents. Enhancement of DNA cleavage potency was observed with those compounds which could interact with DNA through intercalation of the extended aromatic ring or through electrostatic attraction with elec...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-06, Vol.10 (12), p.1321-1325
Main Authors: Basak, Amit, Bdour, Hussam Moh'd, Shain, Jagadish Chandra, Mandal, Subrata, Rudra, Kakali Rani, Nag, Sikha
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
DNA - chemistry
Electrons
General aspects
Hydrolysis
Intercalating Agents - chemistry
Mass Spectrometry
Medical sciences
Pharmacology. Drug treatments
Photochemistry
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Summary:A number of novel N-substituted enediynes (azaenediynes) 1– 4 were synthesized as DNA cleaving agents. Enhancement of DNA cleavage potency was observed with those compounds which could interact with DNA through intercalation of the extended aromatic ring or through electrostatic attraction with electron poor aromatic ring. An acyclic enediyne 5 with a novel phototriggerable device was also synthesized and its DNA-cleaving activity was established.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00237-7