Abstract
Under appropriate electronic modulation, simple diazofluorene analogs recapitulate the DNA cleavage activity of kinamycin D under thiol-based reducing conditions. Achieving DNA cleavage under these reducing conditions is key to anticancer activity, as the most active compound, 1-methoxydiazofluorene, inhibits the proliferation of HeLa cells.
Publication types
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Research Support, N.I.H., Extramural
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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.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Carbazoles / pharmacology
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Cell Proliferation / drug effects
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DNA Damage / drug effects*
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Fluorenes / chemical synthesis*
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Fluorenes / pharmacology
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HeLa Cells
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Humans
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Molecular Mimicry
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Carbazoles
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Fluorenes
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kinamycin D