Abstract
A strategy to site-selectively monoacylate an antitumor saponin OSW-1 was developed using an organotin reagent to rapidly access its derivatives that are useful as chemical probes. 4″-O-Acylated OSW-1 derivatives bearing a fluorophore, an alkyne tag, or biotin were prepared in good yields and were shown to maintain highly cytotoxic activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acylation
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Biotin / chemistry*
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Cell Line, Tumor
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Cholestenones / chemical synthesis*
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Cholestenones / chemistry*
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Humans
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Molecular Structure
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Saponins / chemical synthesis*
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Saponins / chemistry*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Cholestenones
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Saponins
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OSW 1
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Biotin