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以多酚类化合物和多取代苯乙酸类化合物为原料,用“一锅法”合成了24个7-羟基异黄酮类化合物;并从“一锅法”制得的3d,3g经脱除甲基得到两个2’-羟基取代的异黄酮化合物4a和4b.雌激素受体(Estrogen receptors,ERs)的选择性结合活性试验表明:26个化合物(包括4个新化合物3r,3s,3u和3v)中,9个化合物与ERβ相对于ERα的选择性作用强于染料木素(Genistein);发现7,8-二羟基异黄酮类化合物与ERβ相对结合能力高于相应7-羟基异黄酮类化合物;4’取代基对化合物与ERβ结合相对于ERα的选择性影响从大到小为:H>Cl>F>OH;2’,3’及5’位取代基降低异黄酮对ERα和ERβ的亲和性.
Using polyphenols and poly-substituted phenylacetic acids as raw materials, 24 7-hydroxyisoflavonoids were synthesized using “one-pot method”, and from the “one-pot method” Two 2’-hydroxy-substituted isoflavone compounds 4a and 4b were obtained through demethylation.Selective binding activity of estrogen receptors (ERs) showed that 26 compounds including 4 new compounds 3r, 3s, 3u and 3v), the selectivity of 9 compounds with ERβ was stronger than that of ERα with genistein. The relative binding ability of 7,8-dihydroxy isoflavones to ERβ was higher than that of corresponding β- Hydroxyisoflavones; The selectivity of 4 ’substituent on ERβ binding to ERβ is: H> Cl> F> OH. The 2’, 3 ’and 5’ Affinity to ERα and ERβ.