Abstract
Analogs of the anti-tumor agent camptothecin with both closed E-rings (lactone and ether) and open E-rings (reduced acid, hydrazide, and protected Weinreb amide) have been prepared and tested in topoisomerase and cellular assays. The results provide insights into the structural features of the camptothecin E-ring that affect biological activity.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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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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Biological Assay
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Camptothecin / analogs & derivatives*
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Camptothecin / chemical synthesis*
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Camptothecin / chemistry
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Camptothecin / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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DNA / drug effects
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Humans
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Magnetic Resonance Spectroscopy
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Models, Molecular
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Molecular Structure
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Structure-Activity Relationship
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Topoisomerase Inhibitors
Substances
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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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homocamptothecin
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Camptothecin