Abstract
[reaction: see text] Apoptolidin (1) is a promising new therapeutic lead that exhibits remarkable selectivity against cancer cells relative to normal cells. We report the isolation, characterization, solution structure, stability, and biological activity of two new members of this family: apoptolidins B (2) and C (3). These new agents are found to have antiproliferative activity on par with or better than apoptolidin itself in an assay with H292 lung cancer cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Actinobacteria / chemistry*
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Antineoplastic Agents* / chemistry
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Antineoplastic Agents* / isolation & purification
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Antineoplastic Agents* / pharmacology
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Drug Screening Assays, Antitumor
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Humans
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Macrolides* / chemistry
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Macrolides* / isolation & purification
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Macrolides* / pharmacology
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Molecular Structure
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Pyrones* / chemistry
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Pyrones* / isolation & purification
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Pyrones* / pharmacology
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Macrolides
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Pyrones
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apoptolidin A
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apoptolidin B
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apoptolidin C