Abstract
New bisantrene analogues were synthesized, bearing one or two 4,5-dihydro-1H-imidazol-2-yl hydrazone side chains at positions 1,4 or 9 of the anthracene ring system. A 10-azabioisostere was also prepared. The position of substituents in structurally isomeric drugs modulates topoisomerase II poisoning and specificity, along with cytotoxicity.
MeSH terms
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Anthracenes / chemical synthesis
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Anthracenes / metabolism
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Anthracenes / pharmacology
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology
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DNA Damage*
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DNA Topoisomerases, Type II / metabolism*
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Humans
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Tumor Cells, Cultured
Substances
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Anthracenes
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Antineoplastic Agents
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bisantrene
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DNA Topoisomerases, Type II