四氢芴酮作为一类新型雌激素受体β亚型选择性配体的发现。
The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.
作者信息
Wilkening R R, Ratcliffe R W, Tynebor E C, Wildonger K J, Fried A K, Hammond M L, Mosley R T, Fitzgerald P M D, Sharma N, McKeever B M, Nilsson S, Carlquist M, Thorsell A, Locco L, Katz R, Frisch K, Birzin E T, Wilkinson H A, Mitra S, Cai S, Hayes E C, Schaeffer J M, Rohrer S P
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. doi: 10.1016/j.bmcl.2006.03.098. Epub 2006 May 2.
Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.
描述了一系列取代四氢芴酮类似物的合成和衍生化，这些类似物可产生强效的雌激素受体β（ERβ）亚型选择性配体。报道了几种具有与17β-雌二醇相当的ERβ结合亲和力，但对ERα的选择性大于75倍的类似物。
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