Heterocyclic bibenzimidazole derivatives as topoisomerase I inhibitors

A series of 2'-heterocyclic derivatives of 5-phenyl-2,5'-1H-bibenzimidazoles were evaluated for topoisomerase I poisoning activity and cytotoxicity. Topo I poisoning activity was associated with 2'-derivatives that possessed a hydrogen atom capable of hydrogen bond formation, suggesti...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 10; no. 8; pp. 719 - 723
Main Authors SONG JIN, JUNG SUN KIM, SIM, S.-P, LIU, A, PILCH, D. S, LIU, L. F, LAVOIE, E. J
Format Journal Article
LanguageEnglish
Published Oxford Elsevier 17.04.2000
Subjects
Antineoplastic agents
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biological and medical sciences
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General aspects
Heterocyclic Compounds - pharmacology
Medical sciences
Pharmacology. Drug treatments
Spectrum Analysis
Topoisomerase I Inhibitors
Antineoplastic agent
Enzyme
Nitrogen heterocycle
DNA topoisomerase
Enzyme inhibitor
Cytotoxicity
In vitro
Biological activity
Isomerases
Benzimidazole derivatives
Bicyclic compound
Aromatic compound
Chemical synthesis
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Summary:A series of 2'-heterocyclic derivatives of 5-phenyl-2,5'-1H-bibenzimidazoles were evaluated for topoisomerase I poisoning activity and cytotoxicity. Topo I poisoning activity was associated with 2'-derivatives that possessed a hydrogen atom capable of hydrogen bond formation, suggesting that the interatomic distances between such hydrogen atoms and the heteroatoms on the adjacent benzimidazole influence activity.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00087-1