Synthesis and evaluation for uterotrophic and antiimplantation activities of 2-substituted estradiol derivatives
| Autor: | O M, AboulWafa, M M, Mohy el-Din, A, Mohsen, M E, Omar |
|---|---|
| Rok vydání: | 1992 |
| Předmět: |
medicine.medical_specialty
Magnetic Resonance Spectroscopy medicine.drug_class medicine.medical_treatment Clinical Biochemistry Biochemistry Steroid chemistry.chemical_compound Structure-Activity Relationship Endocrinology Internal medicine medicine Animals Embryo Implantation Molecular Biology Semicarbazone Pharmacology Estradiol Organic Chemistry Uterus Biological activity Organ Size 17 beta estradiol Rats chemistry Estrogen Female hormones hormone substitutes and hormone antagonists |
| Zdroj: | Steroids. 57(4) |
| ISSN: | 0039-128X |
| Popis: | Two novel series of 2-substituted estradiol derivatives have been synthesized and evaluated for uterotrophic and antiimplantation activities. Among the compounds tested in the rat, 2-acetylestradiol 17 beta-acetate (1), 2-(3'-dimethylamino-1'-propionyl)estradiol 3,17 beta-diacetate (7), 2-(3'-diethylamino-1'-propionyl)estradiol 3,17 beta-diacetate (8), 2-(3'-piperidino-1'-propionyl)estradiol 3,17 beta-diacetate (9), 1'-(2-estradiol 3,17 beta-diacetate-3'-diethylaminopropionyl thiosemicarbazone (12), and 1'-(2-estradiol 3,17 beta-diacetate)-3'-morpholinopropionyl thiosemicarbazone (14) displayed estrogenic activity. At dosages of 4 microliters/rat/day, none of the tested compounds elicited antiimplantation activity. All compounds shared a similar characteristic: nuclear substitution at the C-2 position of the steroid nucleus, a property previously thought to be markedly inhibitory for estrogenic activity. |
| Databáze: | OpenAIRE |
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