4-取代17β-羟基在-7α-甲基-4-雌烯-3-酮的合成和抗生育活性  

SYNTHESIS OF 4-SUBSTITUTED 17β-HYDROXY-7α-METHYL4-ESTREN-3-ONE AND THEIR 17-ACETATES AS ANTIFERTILITY COMPOUNDS

作　　者：马建标[1] 李振肃[1] 

机构地区：[1]北京医科大学药物化学教研室

出　　处：《药学学报》1990年第1期18-23,共6页Acta Pharmaceutica Sinica

摘　　要：为了寻找抗生育药物,从17β-羟基-7α-甲基-4-雌烯-3-酮经17β-羟基-7α-甲基-4β,5β-环氧雌烷-3-酮合成了七个4-位取代的目标化合物:4,17β-二羟基-7α-甲基-4-雌烯-3-酮及其17-乙酸酯、4-甲氧基-17β-羟基-7α-甲基-4-雌烯-3-酮及其17-乙酸酯、4-氯-17β-羟基-7α-甲基-4-雌烯-3-酮及其17-乙酸酯和4-溴-17β-羟基-7α-甲基-4-雌烯-3-酮。这些化合物均可竞争性地与人蜕膜孕酮受体结合,并能抑制蜕膜细胞的发育,对大鼠具有显著的抗着床活性。Guided by antiprogestational screening results, 4-substituted(4-OH, 4-Cl, 4-Br, and 4-OMe)17β-hydroxy-7α-methyl-4-estren-3-one and their 17-acetate were synthesized via 4β,5β-epoxy-17β-hydroxy-7α-methylestran-3-one from 17β-hydroxy-7α-methyl-4-estren-3-one. Some of these compounds possess strong affinity to human decidual progesterone receptor, inhibit in vitro the growth Of decidual cells, and prevent the implantation in rats at the dose of 1μmol/kg.

关 键 词：甲基睾丸酮 雌烷衍生物 抗着床活性 

分 类 号：R979.23[医药卫生—药品]