title: Synthesis, uterotrophic, and antiuterotrophic activities of some estradiol derivatives containing thiadiazole, thiazoline, and thiazolidinone moieties.
abstract: The effect of structural modification on the biological activity of hormones has been studied on five novel series of estradiol analogs bearing a variety of substituents at the 2-position of the steroidal nucleus. The synthesized compounds include 2-[2-(5-substituted amino-1,3,4-thiadiazol-2-yl)vinyl]estradiol 17 beta-acetate 5-9, 2-aroylmethylestradiols 10-12, 2-[2-aryl-2-(substituted thiocarbamoylhydrazono)ethyl]estradiols 13-18 and their cyclic thiazoline 19-24, and thiazolidinone derivatives 25-30. Among the products, the p-hydroxybenzolmethylestradiol 12 exhibited the highest antiestrogenic activity of 63%. It also elicited 34% of the uterotrophic activity of estradiol.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Egypt.
authors.forename: A A
authors.initials: AA
authors.lastname: el-Tombary
mesh_terms: D000818:Animals; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D009682:Magnetic Resonance Spectroscopy; D009929:Organ Size / Q000187:drug effects; D051381:Rats; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D014599:Uterus / Q000033:anatomy & histology / Q000187:drug effects*
chemical_list: D013830:Thiadiazoles; D013844:Thiazoles; D004958:Estradiol