Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 13, Pages 4007-4019Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm9003973
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Funding
- Fundacao para a Ciencia e Tecnologia (FCT), Portugal [SFRH/BD/18263/2004]
- Fundação para a Ciência e a Tecnologia [SFRH/BD/18263/2004] Funding Source: FCT
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A library of diastereomerically pure epoxysterols, prepared by combining chemical and enzymatic methodologies, was evaluated for cytotoxicity toward human cancer and noncancer cell lines. Unsaturated steroids were oxidized by magnesium bis(monoperoxyphthal ate) hexahydrate in acetonitrile, and the resulting epimeric epoxides were enzymatically separated using Novozym 435 or lipase AY. Some of the synthesized epoxysterols have potent cytotoxicity and higher activity on cancer cell lines HT29 and LAMA-84.
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