Synthesis and Biological Activity of Oxidation Products of the Antiprogestine Mifepristone |
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| Authors: | Rainer Strommer Wolfgang Strauss Helmut Emmert Reinhard Sailer Rudolf Steiner Eva Reisinger Ernst Haslinger Hans W. Schramm |
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| Affiliation: | Institut fü Pharmazeutische Chemie, Universit?t Graz, A-8010 Graz, Austria, AT
Institut fü Lasertechnologien in der Medizin und Me?technik an der Universit?t Ulm, D-89081 Ulm, Germany, DE
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| Abstract: | Summary. Selenium dioxide oxidation allows the selective introduction of a hydroxyl group at position 6 of the steroid skeleton of the antihormone (11β, 17β)-11-(4-dimethylamino-phenyl)-17-hydroxyl-17-(1-propynyl)-estra-4,9-dien-3-one (mifepristone, RU 486) and leads in a one-step procedure to two diastereomeric oxidation products. Their structure (6α- and 6β-hydroxy-mifepristone) was determined by NMR spectroscopy. The antiprogestinic activity of the oxidation products is comparable to that of mifepristone. Received August 25, 2000. Accepted (revised) October 24, 2000 |
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| Keywords: | . Anti-hormones Mifepristone NMR spectroscopy Oxidation Cancer therapy. |
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