Abstract
A series of A-ring and E-ring analogues of the natural product luotonin A, a known topoisomerase I poison, was evaluated for growth inhibition in human carcinoma and leukemia cell lines. Rational design of structures was based on analogues of the related alkaloid camptothecin, which has been demonstrated to exert cytotoxic effects by the same mechanism of action. When compared to luotonin A, several compounds exhibited an improved topoisomerase I-dependent growth inhibition of a human leukemia cell line.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Humans
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Magnetic Resonance Spectroscopy
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Pyrroles / chemical synthesis*
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Pyrroles / pharmacology*
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Quinones / chemical synthesis*
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Quinones / pharmacology*
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Spectrometry, Mass, Electrospray Ionization
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Topoisomerase I Inhibitors*
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Topoisomerase II Inhibitors*
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Pyrroles
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Quinones
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Topoisomerase I Inhibitors
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Topoisomerase II Inhibitors
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luotonin A