Abstract

A series of 4a-methyl-3,4,4,4a-9-tetrahydrophenanthrene-2-carboxylic acids and 2-phosphinic acids has been prepared and evaluated in vitro as inhibitors of human recombinant steroid 5α-reductase. 7-Chloro-4a-methyl-3,4,4,4a-9-tetrahydrophenanthrene-2-carboxylic acid 5, is a marginally selective inhibitor of human type 2 steroid 5α-reductase (K i,app = 260 nM). The phosphinic acid compounds, 8 and 9, are weak inhibitors of types 1 and 2 steroid 5α-reductase.

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