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

B T Ngatcha; V Luu-The; D Poirier

doi:10.1016/s0960-894x(00)00517-5

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.

Authors

B T Ngatcha¹, V Luu-The, D Poirier

Affiliation

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

17-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
Androsterone / chemistry*
Cell Line
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Humans

Substances

Enzyme Inhibitors
Androsterone
17-Hydroxysteroid Dehydrogenases
3 (or 17)-beta-hydroxysteroid dehydrogenase