Efficient Chemoenzymatic Synthesis, Cytotoxic Evaluation, and SAR of Epoxysterols
Journal of Medicinal Chemistry2009Vol. 52(13), pp. 4007–4019
Citations Over TimeTop 12% of 2009 papers
Abstract
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(monoperoxyphthalate) 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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