Abstract
Several benzo[c]pyrido[2,3,4-kl]acridines bearing different substituents on the A and E rings were synthesized and evaluated for their capacity to bind to DNA and to inhibit DNA topoisomerases. Potent cytotoxic compounds were discovered but no strict correlation with their DNA binding affinity and effects on topoisomerases were observed. DNA is one but not the unique target of these compounds.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acridines / chemistry*
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Acridines / metabolism
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Acridines / pharmacology*
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Animals
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology*
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Cattle
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DNA / metabolism
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DNA Topoisomerases / chemistry
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / metabolism
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Enzyme Inhibitors / pharmacology
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Humans
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Inhibitory Concentration 50
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Male
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Nucleic Acid Conformation
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Nucleic Acid Denaturation
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Prostatic Neoplasms / drug therapy
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Topoisomerase Inhibitors
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Tumor Cells, Cultured
Substances
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Acridines
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Antineoplastic Agents
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Enzyme Inhibitors
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Topoisomerase Inhibitors
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DNA
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calf thymus DNA
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DNA Topoisomerases