Abstract
Several 2'-aryl-5-substituted-2,5'bi-1H-benzimidazole derivatives were synthesized and evaluated as topoisomerase I poisons and for their cytotoxicity toward the human lymphoblast cell line RPMI 8402. This study focused on 18 2,5'-bi-1H-benzimidazole derivatives which contained either a 5-cyano, a 5-(aminocarbonyl), or a 5-(4-methylpiperazinyl) group. Among these bibenzimidazoles, the pharmacological activity of 2'-phenyl derivatives and the influence of the different positional isomers of either a 2'-tolyl group or a 2'-naphthyl moiety on cytotoxicity and topoisomerase I inhibitory activity were determined.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / toxicity
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / pharmacology*
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Benzimidazoles / toxicity
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Cell Line
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Drug Design
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Enzyme Inhibitors / toxicity
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Humans
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Magnetic Resonance Spectroscopy
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Molecular Structure
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Structure-Activity Relationship
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Topoisomerase I Inhibitors*
Substances
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Antineoplastic Agents
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Benzimidazoles
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Enzyme Inhibitors
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Topoisomerase I Inhibitors