Chemical synthesis, characterisation and biological evaluation of lactonic-estradiol derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase type 1

- 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%).