| Literature DB >> 2308144 |
D A Holt1, M A Levy, D L Ladd, H J Oh, J M Erb, J I Heaslip, M Brandt, B W Metcalf.
Abstract
A series of 17 beta-carbamoyl-1,3,5(10)-estratriene-3-carboxylic acids has been prepared and evaluated in vitro as inhibitors of human and rat prostatic steroid 5 alpha-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.Entities:
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Year: 1990 PMID： 2308144 DOI： 10.1021/jm00165a009
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446