Abstract
Analogues of the potent cytotoxic saponin OSW-1 were prepared from the readily available steroidal 16β,17α,22-triol. The new 22-deoxo-23-oxa analogues of OSW-1 were screened against eight cancer cell lines and normal human fibroblasts. The analogues proved to be slightly less active than OSW-1 but also less toxic to normal cells. They induce concentration- and time-dependent apoptosis of mammalian cancer cells with caspase-3 activation.
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 / chemistry
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Antineoplastic Agents / pharmacology
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Apoptosis
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Caspase 3 / metabolism
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Caspase 7 / metabolism
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Cell Cycle / drug effects
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Cell Line, Tumor
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Cholestenones / chemical synthesis*
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Cholestenones / chemistry
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Cholestenones / pharmacology
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Drug Screening Assays, Antitumor
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Enzyme Activation
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Fibroblasts / drug effects
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Humans
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Saponins / chemical synthesis*
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Saponins / chemistry
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Saponins / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Cholestenones
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Saponins
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OSW 1
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Caspase 3
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Caspase 7