Abstract
New antitumor 12-alkoxy-benzo[c]phenanthridinium derivatives were obtained in high yields through multistep syntheses. Analysis of DNA binding and human DNA topoisomerase I inhibitory activities demonstrates that new compounds, combining 2, 6, and 12 substitutions, interact strongly with DNA and exhibit important topoisomerase I inhibition. The cytotoxicities against solid tumor cell lines are also determined and compared with those for fagaronine and ethoxidine.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkaloids / pharmacology
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Alkanes / chemical synthesis
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Alkanes / chemistry
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Alkanes / pharmacology*
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Benzophenanthridines
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DNA / drug effects*
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DNA / metabolism
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DNA Topoisomerases, Type I / metabolism
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / pharmacology
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Humans
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Phenanthridines / chemical synthesis
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Phenanthridines / chemistry
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Phenanthridines / pharmacology*
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Topoisomerase I Inhibitors*
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Tumor Cells, Cultured
Substances
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Alkaloids
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Alkanes
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Antineoplastic Agents
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Benzophenanthridines
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Enzyme Inhibitors
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Phenanthridines
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Topoisomerase I Inhibitors
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ethoxidine
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fagaronine
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DNA
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DNA Topoisomerases, Type I