Novel steroidal pure antiestrogens |
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| Authors: | J Bowler T J Lilley J D Pittam A E Wakeling |
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| Institution: | Research Department 1, ICI Pharmaceuticals, Macclesfield, Cheshire, UK. |
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| 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. |
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