Schubert G, Ponsold K, Hillesheim H G, Koch M
Pharmazie. 1980 Aug;35(8):453-7.
The preparation of the 17 beta-carbamoyl derivatives 4 and of the 17 beta-carbonic acid esters 5 from 15 beta,16 beta-epoxy-3-methoxyoestra-1,3,5(10)-triene-17 beta-ol (3a), and the subsequent opening of the 15 beta,16 beta-epoxy group resulting in 15 beta,16 alpha,17 beta-trisubstituted oestratrienes 6 are described. The influences of several substitutents in the positions 15 and 16 and of the 17 beta-hydroxy group and derivatives thereof on the uterotropic and cholesterol-lowering activities were investigated in rats after oral application. A correlation between the cholesterol-lowering and the uterotropic activity could be established. Activity dissociation was not achieved.
描述了由15β,16β-环氧-3-甲氧基雌-1,3,5(10)-三烯-17β-醇(3a)制备17β-氨基甲酰基衍生物4和17β-碳酸酯5,以及随后15β,16β-环氧基团的开环生成15β,16α,17β-三取代雌三烯6的过程。口服给药后,研究了15和16位的几个取代基以及17β-羟基及其衍生物对大鼠子宫促生长活性和降胆固醇活性的影响。可以建立降胆固醇活性与子宫促生长活性之间的相关性。未实现活性解离。