Synthesis of potential antiprogestogens.
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.
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D066298:In Vitro Techniques; D011372:Progestins / Q000037:antagonists & inhibitors* / Q000502:physiology; D011817:Rabbits; D011956:Receptors, Cell Surface / Q000187:drug effects; D013329:Structure-Activity Relationship
D011372:Progestins; D011956:Receptors, Cell Surface