diastereomers. The binding affinity of these compounds to the calf uterine estrogen receptor was measured relative to that of [3H]estradiol by a competitive binding assay. All test compounds showed relative binding affinity (RBA) values between 32 and less than 0.01% that of estradiol. Only meso-3,4-bis(2,4-dihydroxyphenyl)hexane (16) showed an estrogen receptor binding affinity comparable to that
描述了对称的3,3'-和2,2'-双取代的内消旋己烯醇衍
生物的合成[3,3'-取代基:OH(1),F(2),Cl(3),Br(4),I (5),
CH2N(
CH3)2(6), (7),CH2O (8),CH2O (9),CH2OH(10),
NO2(11),NH2(12),N( )2(13 ),CO (14)和
C2H5(15);2,2'-取代基:OH(16),F(17),Cl(18),Br(19), (20)和 (21)]。1-3的合成是通过将
苯乙酮与TiCl4 / Zn还原偶联并随后将顺式3,4-二苯基己基-3-烯氢化而完成的。通过取代
己烯雌酚获得化合物4-15,而通过将1-苯基-1-
丙醇与TiCl3 / LiAlH4偶联并分离内消旋非对映异构体来合成化合物16-21。通过竞争性结合测定法测量了这些化合物对小牛子宫
雌激素受体的结合亲和力与[3H]
雌二醇的结合亲