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

  • Bioorg Med Chem Lett. 2000 Nov 20;10(22):2533-6. doi: 10.1016/s0960-894x(00)00517-5.
B T Ngatcha  1 ,  V Luu-The ,  D Poirier
Affiliations
  • 1. Medicinal Chemistry Division, Oncology and Molecular Endocrinology Research Center, Laval University Medical Center (CHUL) and Laval University, Quebec, Canada.
PMID: 11086723 DOI: 10.1016/s0960-894x(00)00517-5
Abstract

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 17beta-hydroxysteroid dehydrogenase, a key enzyme of steroidogenesis, which catalyzes the transformation of androstenedione to steroid active androgen testosterone.