title: Novel steroidal pure antiestrogens.
abstract: A series of steroidal estrogen antagonists with no intrinsic estrogenicity in rat uterotrophic-antiuterotrophic tests has been discovered. The compounds are derivatives of estradiol containing amidoalkyl side chains at the 7 alpha-position. The most potent compounds are N-n-butyl-N-methyl-11-(3,17 beta-dihydroxyestra- 1,3,5(10)-trien-7 alpha-yl) undecanamide and N-2,2,3,3,4,4,4-heptafluorobutyl-N-methyl-11-(3,17 beta-dihydroxyestra- 1,3,5(10)-trien-7 alpha-yl) undecanamide. Structure activity relationships are discussed.
authors.affiliation: Research Department 1, ICI Pharmaceuticals, Macclesfield, Cheshire, UK.
authors.forename: J
authors.initials: J
authors.lastname: Bowler
authors.forename: T J
authors.initials: TJ
authors.lastname: Lilley
authors.forename: J D
authors.initials: JD
authors.lastname: Pittam
authors.forename: A E
authors.initials: AE
authors.lastname: Wakeling
mesh_terms: D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D004965:Estrogen Antagonists; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D004965:Estrogen Antagonists