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Synthesis and biological activity of 4-methylestradiol
Authors:X D Qian  Y J Abul-Hajj
Affiliation:Department of Medicinal Chemistry and Pharmacognosy, University of Minnesota, Minneapolis 55455.
Abstract: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.
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