Bowler J, Lilley T J, Pittam J D, Wakeling A E
Research Department 1, ICI Pharmaceuticals, Macclesfield, Cheshire, UK.
Steroids. 1989 Jul;54(1):71-99. doi: 10.1016/0039-128x(89)90076-7.
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.
已发现一系列在大鼠子宫营养-抗子宫营养试验中无内在雌激素活性的甾体雌激素拮抗剂。这些化合物是雌二醇的衍生物，在7α位含有酰胺烷基侧链。最有效的化合物是N-正丁基-N-甲基-11-(3,17β-二羟基雌甾-1,3,5(10)-三烯-7α-基)十一酰胺和N-2,2,3,3,4,4,4-七氟丁基-N-甲基-11-(3,17β-二羟基雌甾-1,3,5(10)-三烯-7α-基)十一酰胺。讨论了构效关系。
