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

Authors
Ngatcha, BT Luu-The, V Poirier, D
Citation
Bt. Ngatcha et al., Androsterone 3 beta-substituted derivatives as inhibitors of type 3 17 beta-hydroxysteroid dehydrogenase, BIOORG MED, 10(22), 2000, pp. 2533-2536
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
22
Year of publication
2000
Pages
2533 - 2536
Database
ISI
SICI code
0960-894X(20001120)10:22<2533:A3BDAI>2.0.ZU;2-#
Abstract
Androsterone derivatives substituted at position 3 were synthesized startin g from dihydrotestosterone in a short sequence of reactions. They proved to be potent inhibitors (IC50 = 57-147 nM) of type 3 17 beta -hydroxysteroid dehydrogenase, a key enzyme of steroidogenesis, which catalyzes the transfo rmation of androstenedione to steroid active androgen testosterone. (C) 200 0 Elsevier Science Ltd. All rights reserved.