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Inhibitory effects of fluorine-substituted estrogens on the activity of 17beta-hydroxysteroid dehydrogenases
Dominga Deluca1, Gabriele Möller, Andrea Rosinus
1GSF-National Research Center for Environment and Health, Institute of Experimental Genetics, Genome Analysis Center, Ingolstädter Landstr. 1, 85764 Neuherberg, Germany.
Abstract:
In search for new inhibitors of human 17beta-hydroxysteroid dehydrogenase type 1 (h17beta-HSD1) a specific group of steroids with interesting properties including novel compounds was investigated. Several estratriene derivatives with fluorine-substitution in position 17 of the steroidal scaffold were synthesised and tested in vitro towards recombinant h17beta-HSD1, 2, 4, 5 and 7. Moderate, mostly unselective inhibitors of h17beta-HSD1 and h17beta-HSD2 and a selective inhibitor of h17beta-HSD5 were identified. The structure-activity relationship with respect to inhibitory strengths and selectivity of these compounds on five h17beta-HSDs is discussed.
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