Synthesis and evaluation of 17α-E-20-(heteroaryl)norpregn-1,3,5(10),20 tetraene-3,17β-diols [17α-(heteroaryl)vinyl estradiols] as ligands for the estrogen receptor-α ligand binding domain (ERα-LBD).
Synthesis and evaluation of 17α-E-20-(heteroaryl)norpregn-1,3,5(10),20 tetraene-3,17β-diols [17α-(heteroaryl)vinyl estradiols] as ligands for the estrogen receptor-α ligand binding domain (ERα-LBD).
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17α-E-20-(杂芳基)norpregn-1,3,5(10),20 四烯-3,17β-二醇 [17α-(杂芳基)乙烯基雌二醇] 作为雌激素受体配体的合成和评价-
DOI：
10.1016/j.bmcl.2011.12.003
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发表时间：
2012
影响因子：
2.7
通讯作者：
Hanson,RobertN
中科院分区：
文献类型：
--
作者：
Olmsted,SandraL;Tongcharoensirikul,Pakamas;McCaskill,Emmett;Gandiaga,Karla;Labaree,David;Hochberg,RichardB;Hanson,RobertN
A series of 17α-(heteroaryl)vinyl estradiols was prepared to evaluate the influence of heteroatom on the affinity and efficacy of estrogenic ligands for the estrogen receptor-alpha ligand binding domain (ERα-LBD). The products demonstrated reduced binding affinity compared to the parent 17α-E-phenylvinyl estradiol, but the binding was relatively independent of the heteroatom. The greatest influence of the heteroatom was evident in the efficacy of the compounds as the thienyl derivatives 2f,g were more potent than either the pyridyl 2b–d or pyrimidinyl 2e analogs. The results suggest that a subtle interplay of interactions between the ligands and the receptor influences the biological response.
