Journal of Medicinal Chemistry p. 937 - 942 (1990)
Update date:2022-07-30
Topics:
Holt
Levy
Ladd
Oh
Erb
Heaslip
Brandt
Metcalf
A series of 17β-carbamoyl-1,3,5(10)-estratriene-3-carboxylic acids has been prepared and evaluated in vitro as inhibitors of human and rat prostatic steroid 5α-reductase (EC 1.3.1.30). Potent inhibition of the human enzyme, in particular, was observed and preliminary studies using rat enzyme suggest that the inhibition results from the formation of an enzyme-NADP+-inhibitor complex. The compounds were synthesized from estrone, generally employing a differentiated bis-triflate carbonylation strategy.
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Doi:10.1007/BF00472480
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