Regioselective synthesis and estrogenicity of (±)-8-alkyl-5, 7-dihydroxy-4-(4-hydroxyphenyl)-3, 4-dihydrocoumarins

…, M Van Cleemput, F Comhaire, D De Keukeleire

文献索引：Roelens, Frederik; Huvaere, Kevin; Dhooge, Willem; Van Cleemput, Marjan; Comhaire, Frank; De Keukeleire, Denis European Journal of Medicinal Chemistry, 2005 , vol. 40, # 10 p. 1042 - 1051

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被引用次数: 51

摘要

Nine new (±)-8-alkyl-5, 7-dihydroxy-4-(4-hydroxyphenyl)-3, 4-dihydrocoumarins have been synthesized from 2, 4, 6-trimethoxybenzaldehyde via a short, efficient, and regioselective pathway, together with the unsubstituted analogue (±)-5, 7-dihydroxy-4-(4-hydroxyphenyl)-3, 4-dihydrocoumarin. The compounds were tested for estrogenic activity using a yeast-based estrogen screen. Weak estrogenicity was determined for seven members of the series.