Steroidal A ring aryl carboxylic acids: a new class of steroid 5.alpha.-reductase inhibitors
| Autor: | Jill M. Erb, H.-J. Oh, Dennis A. Holt, David L. Ladd, Brian W. Metcalf, Mark Alan Levy, Julie I. Heaslip, Martin Brandt |
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| Rok vydání: | 1990 |
| Předmět: |
Male
Stereochemistry medicine.drug_class medicine.medical_treatment Carboxylic acid Carboxylic Acids Estrone Carboxamide Reductase Steroid Structure-Activity Relationship chemistry.chemical_compound 5 Alpha-Reductase Inhibitor 5-alpha Reductase Inhibitors Drug Discovery medicine Animals Humans chemistry.chemical_classification biology Prostate Rats Enzyme chemistry Biochemistry Enzyme inhibitor biology.protein Molecular Medicine |
| Zdroj: | Journal of Medicinal Chemistry. 33:937-942 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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