First Inhibitors of the Steroidogenic Enzyme Type 7 17β-Hydroxysteroid Dehydrogenase

E. Bellavance; V. Luu-The; D. Poirier

doi:10.2174/1570180043398867

ISSN: 1570-1808
E-ISSN: 1875-628X

First Inhibitors of the Steroidogenic Enzyme Type 7 17β-Hydroxysteroid Dehydrogenase
Authors: E. Bellavance¹, V. Luu-The² and D. Poirier³
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¹ Medicinal Chemistry Division, Oncology and Molecular Endocrinology Research Center, Centre Hospitalier Universitaire de Quebec (CHUQ), Pavillon CHUL, T3-67, 2705 Laurier Boulevard, Quebec , G1V 4G2, Canada ² Medicinal Chemistry Division, Oncology and Molecular Endocrinology Research Center, Centre Hospitalier Universitaire de Quebec (CHUQ), Pavillon CHUL, T3-67, 2705 Laurier Boulevard, Quebec , G1V 4G2, Canada ³ Medicinal Chemistry Division, Oncology and Molecular Endocrinology Research Center, Centre Hospitalier Universitaire de Quebec (CHUQ), Pavillon CHUL, T3-67, 2705 Laurier Boulevard, Quebec , G1V 4G2, Canada
Source: Letters in Drug Design & Discovery, Volume 1, Issue 3, Jul 2004, p. 194 - 197
DOI: https://doi.org/10.2174/1570180043398867
- Available online: 01 Jul 2004

Abstract

We present the SAR study that led us to identification of the first inhibitors of type 7 17β- hydroxysteroid dehydrogenase (17β-HSD). The conversion of E1 into E2 is reduced by nearly 90 % by 17β-(Nalkylformamido)- 4-methyl-4-aza-5α-androstan-3-one compounds bearing a side chain containing 7 to 10 carbon atoms when tested at 0.3 μM.

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2004-07-01

2025-09-28

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Article Type: Review Article

Keyword(s): 4-aza-steroids; enzyme; hydroxysteroid dehydrogenase; inhibitors; sar; steroidogenesis

First Inhibitors of the Steroidogenic Enzyme Type 7 17β-Hydroxysteroid Dehydrogenase

Abstract

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