Novel steroidal pure antiestrogens.
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.
Bowler
J
J
Research Department 1, ICI Pharmaceuticals, Macclesfield, Cheshire, UK.
Lilley
T J
TJ
Pittam
J D
JD
Wakeling
A E
AE
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D004965:Estrogen Antagonists; D051381:Rats; D013329:Structure-Activity Relationship
D004965:Estrogen Antagonists