Abstract
Analogues of the natural product noscapine were synthesized, and their potential as antitumor agents were examined. The discovery of a novel regio- and stereoselective O-demethylation led to the synthesis of several O-alkylated analogues that induced an unexpected S-phase arrest of mammalian cells. Compound 4a was the most potent analogue inhibiting cell proliferation at an EC(50) of 1.9 microM.
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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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Humans
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Noscapine / analogs & derivatives*
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Noscapine / chemical synthesis*
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Noscapine / chemistry
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Noscapine / pharmacology
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S Phase / drug effects*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Noscapine