Abstract
A series of A-ring unsaturated 3-nitrosteroids has been prepared and assayed in vitro as inhibitors of steroid 5α-reductase. One of these compounds, 3-nitro-5α-androst-3-ene-17β-diisopropylcarboxamide ( 4), inhibits the human enzyme with a K i of 50 nM and exhibits competitive inhibition versus testosterone. Potent oral activity of 4 was demonstrated in cynomolgus monkeys.
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