Androsterone 3β-substituted derivatives as inhibitors of type 3 17β-hydroxysteroid dehydrogenase

Androsterone derivatives substituted at position 3 were synthesized starting from dihydrotestosterone in a short sequence of reactions. They proved to be potent inhibitors (IC50=57–147 nM) of type 3 17β-hydroxysteroid dehydrogenase, a key enzyme of steroidogenesis, which catalyzes the transformation of androstenedione to steroid active androgen testosterone.