Synthesis of potential antiprogestogens
| Autor: | Lars Terenius, Robert W. Brueggemeier, V. V. Ranade, Bernardo Beyer, Raymond E. Counsell |
|---|---|
| Rok vydání: | 1976 |
| Předmět: |
medicine.medical_specialty
Chemical Phenomena Stereochemistry Clinical Biochemistry Uterus Receptors Cell Surface In Vitro Techniques Biology Binding Competitive Biochemistry Structure-Activity Relationship Endocrinology Low affinity Internal medicine medicine Animals Receptor Molecular Biology Alkyl Pharmacology chemistry.chemical_classification Genitalia.female Organic Chemistry Chemistry Cytosol medicine.anatomical_structure chemistry Hormone receptor Female Rabbits Progestins Hormone |
| Zdroj: | Steroids. 27:123-131 |
| ISSN: | 0039-128X |
| Popis: | Acylated derivatives of 17 alpha-hydroxyprogesterone were prepared in order to test the hypothesis that dialkylamino alkyl moieties have the effect of transforming progestogens into antiprogestogens. This approach has been successful with certain estrogens. Compounds with other functional groups were synthesized to determine whether these might exert binding influence outside the area occupied by progesterone itself. The compounds were tested for competitive affinity against tritiated progesterone and receptor from rabbit uterus cytosol. The low affinity of all derivatives makes it unlikely that they would be active as antiprogestational agents.The synthesis of potential antiprogestogens is described. Acylated derivatives of 17alpha-hydroxyprogesterone were prepared to test the hyp othesis that dialkylamino alkyl moieties have the effect of transforming progestogens into antiprogestogens. Compounds with other functional groups were synthesized to determine if they might exert binding influence outside the area occupied by progesterone itself. Each compound was tested for competitive affinity against tritiated progester one and receptor from rabbit uterus cytosol. All the derivatives showed low affinity which makes it unlikely that they would be active antiprogestational agents. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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