Abstract
Introducing a spiro-γ-lactone at position 17 of an estradiol nucleus provokes a potent inhibition of 17β-hydroxysteroid dehydrogenase (17β-HSD) type 2. Synthesis of such a compound, namely 6 (3-hydroxy-19-nor-17α-pregna-1,3,5(10)-triene-21,17β-carbolactone), was performed in five steps, starting with estrone. Inhibition analysis of this compound, the first inhibitor of 17β-HSD, using human placental microsomes and 4-androstene-3,17-dione as substrate shows a Ki value of 0.25 μM.
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