Article ID Journal Published Year Pages File Type
8339134 The Journal of Steroid Biochemistry and Molecular Biology 2013 32 Pages PDF
Abstract

- Lactone- and lactol-estradiol derivatives were synthesized and characterized.
- Lactone E-ring was diversified by adding a hydroxymethyl, a methylcarboxylate, a carboxy or an allyl group.
- A chemical approach was developed to introduce a chemical group on hindered beta-steroid face.
- Lactone and lactol derivatives inhibited 17β-HSD1 (34-60%) similarly as the natural substrate estrone (53%).
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