Qian X D, Abul-Hajj Y J
Department of Medicinal Chemistry and Pharmacognosy, University of Minnesota, Minneapolis 55455.
J Steroid Biochem. 1990 May;35(6):745-7. doi: 10.1016/0022-4731(90)90318-m.
The synthesis of 4-methylestradiol (4-ME2) was carried out by reductive aromatization of 4-methyl-1,4-androstadiene-3-one-17 beta-ol. The relative binding affinity of 4-ME2 was found to be 10 and 25% of estradiol at 0 and 25 degrees C, respectively. 4-ME2 had considerably weaker uterotrophic activity relative to estrone and was found to have no antiuterotrophic activity.
4-甲基雌二醇（4-ME2）通过4-甲基-1,4-雄甾二烯-3-酮-17β-醇的还原芳构化反应合成。结果发现，4-ME2在0℃和25℃时的相对结合亲和力分别为雌二醇的10%和25%。相对于雌酮，4-ME2的子宫营养活性明显较弱，且发现其没有抗子宫营养活性。
