Azasteroids as inhibitors of rat prostatic 5. alpha.-reductase

GH Rasmusson, GF Reynolds, T Utne…

Index: Rasmusson, Gary H.; Reynolds, Glenn F.; Utne, Torleif; Jobson, Ronald B.; Primka, Raymond L.; et al. Journal of Medicinal Chemistry, 1984 , vol. 27, # 12 p. 1690 - 1701

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Citation Number: 178

Abstract

A series of A-ring heterocyclic steroids has been prepared and tested for inhibition of rat prostatic steroid 5a-reductase in vitro. Strikingly high inhibitory activity was found with a group of 17p-substituted 4-methyl-4-aza-5aandrostan-3-ones. These compounds were prepared from 3-keto-A4-precursors by oxidative (0, or NaI04-KMn04) A-ring cleavage followed, in turn, by ring closure with an amine and hydrogenation over platinum catalyst. ...