11,21-Bisphenyl-19-norpregnane derivatives are selective antiglucocorticoids
| Autor: | H. van der Voort, W. Schuts, W. Schoonen, R. Gebhard |
|---|---|
| Rok vydání: | 1997 |
| Předmět: |
medicine.medical_treatment
Organic Chemistry Clinical Biochemistry Antagonist Pharmaceutical Science Nanotechnology Biochemistry Combinatorial chemistry Chemical synthesis Steroid chemistry.chemical_compound Glucocorticoid receptor chemistry Drug Discovery Progesterone receptor medicine Molecular Medicine Selectivity Molecular Biology Enone Glucocorticoid medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 7:2229-2234 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(97)00397-1 |
| Popis: | An efficient eight-step synthesis of 11,21-bisphenyl-19-norpregnane derivatives (10) starting from 19-norandrosta-4,9-diene-3,17-dione (5) is described. It is shown that specific combinations of polar substitutions on the 11- and the 21-phenylring in compounds (10) lead to selective antiglucocorticoids with relative high binding to the glucocorticoid receptor and almost negligible binding to the progesterone receptor. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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