Synthesis and biological properties of 17.alpha.-furylestradiol and dihydroequilin derivatives
| Autor: | Clara Revesz, Yvon Lefebvre |
|---|---|
| Rok vydání: | 1975 |
| Předmět: |
Dihydroequilin
Estranes Alpha (ethology) Estrone Pharmacology Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Animals Structure–activity relationship Furans Hydroxysteroids Dose-Response Relationship Drug Estradiol Uterus Organ Size Mestranol 17-Ketosteroids Rats Equilin Dose–response relationship chemistry Acetylation Molecular Medicine Female medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 18:217-219 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00236a027 |
| Popis: | A series of 17alpha-furylestradiol and dihydroequilin derivatives was synthesized by reacting the appropriate 3-substituted estrone and equilin with 2- or 3-furyllithium. The oral estrogenic activity of the compounds was compared with that of mestranol. In the Allen-Doisy test, the 17alpha-(3-furyl) analogs were 4-19 times as potent orally as the standard in rats but they were less active in mice. Acetylation of the 17-alcohol or replacement of the 3-furyl by a 2-furyl group produced a decrease in activity. In the mouse uterotrophic assay in mice the compounds were less effective than mestranol and exhibited very shallow dose-response curves. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|