225245-08-9Relevant academic research and scientific papers
Androsterone 3α-ether-3β-substituted and androsterone 3β-substituted derivatives as inhibitors of type 3 17β-hydroxysteroid dehydrogenase: Chemical synthesis and structure - Activity relationship
Ngatcha, Béatrice Tchédam,Luu-The, Van,Labrie, Fernand,Poirier, Donald
, p. 5257 - 5268 (2007/10/03)
Type 3 17β-hydroxysteroid dehydrogenase (17β-HSD) is involved in the biosynthesis of androgen testosterone. To produce potent inhibitors of this key steroidogenic enzyme, we prepared a series of androsterone (ADT) derivatives by adding a variety of substi
Inhibitors of type 5 and type 3 17β-hydroxysteroid dehydrogenase and methods for their use
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, (2008/06/13)
Novel methods of medical treatment and/or inhibition of development of diseases are disclosed for diseases that are sensitive to androgenic or estrogenic activity. The treatments utilize inhibitors of type 5 and/or type 3 17β-hydroxysteroid dehydrogenase. Novel inhibitors of type 5 17β-hydroxysteroid dehydrogenase are also disclosed, as are novel inhibitors of type 3 17β-hydroxysteroid dehydrogenase.
Androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase.
Ngatcha,Luu-The,Poirier
, p. 2533 - 2536 (2007/10/03)
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 s
Diastereoselective addition of organomagnesium reagents to 17β-TBDMS- dihydrotestosterone
Ngatcha, Beatrice Tchedam,Poirier, Donald
, p. 1065 - 1074 (2007/10/03)
Several alkylations of the C3-carbonyl of 17β-TBDMS-DHT (1) with Grignard reagents were performed to obtain a series of potential inhibitors of androgen formation. It has been found that, depending on the nucleophilicity of the Grignard reagent used, there was a difference in the diastereoselectivity. The stronger reagents proceeded preferentially through the equatorial attack, while the weaker ones proceeded through the axial attack.
