9,11-Seco steroids. Attempt to separate biological activities via ring cleavage
| Autor: | John H. Dygos, Richard L. Aspinall, Leland J. Chinn, Robert E. Ranney, Stanley E. Mares |
|---|---|
| Rok vydání: | 1974 |
| Předmět: |
Male
Stereochemistry Estranes Research methodology Freund's Adjuvant Anti-Inflammatory Agents Estrone Pharmacology Carrageenan Cleavage (embryo) Arthritis Rheumatoid Mice Structure-Activity Relationship Health services chemistry.chemical_compound Contraceptive Agents Cyclopentanol Pregnancy Drug Discovery Animals Edema Secosteroids Bond cleavage Chemistry Uterus Estrogen Antagonists Organ Size Rats Cholesterol Fertility Molecular Medicine Female Rabbits Hormone |
| Zdroj: | Journal of Medicinal Chemistry. 17:351-354 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00249a021 |
| Popis: | A series of seco steroids with rings A and B aromatic were synthesized in order to determine the effect which scission of the 911-bond had on biological activities. The desired effect was to suppress the feminizing of the estrogens without concomitant loss of other biological activities. One compound 5a(plus or minus-trans-anti-2-( 2-hydroxy-2- methypropyl)-1-ethynyl-3-(6-methoxy-2-naphthyl)cyclopentanol) was found to have antiostrogen antifertility and antiinflammatory properties with an estrogenic activity approximately .003% that of estrone. Compound 5a showed neither progestational or antiprogestational activity. |
| Databáze: | OpenAIRE |
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