Henke B R, Drewry D H, Jones S A, Stewart E L, Weaver S L, Wiethe R W
Department of Medicinal Chemistry, Glaxo Wellcome Research and Development, Five Moore Drive, 27709, Research Triangle Park, NC, USA.
Bioorg Med Chem Lett. 2001 Jul 23;11(14):1939-42. doi: 10.1016/s0960-894x(01)00321-3.
We have prepared a novel series of 2-amino-4,6-diarylpyridines that function as ligands of estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta). These compounds bind to both ERalpha and ERbeta with a modest selectivity for the alpha subtype. The most potent of these analogues, compound 19, has a K(i)=20nM at ERalpha. These molecules represent a novel template for designing potentially useful ligands for the estrogen receptor.
我们制备了一系列新型的2-氨基-4,6-二芳基吡啶，它们可作为雌激素受体α（ERα）和雌激素受体β（ERβ）的配体。这些化合物能同时与ERα和ERβ结合，对α亚型具有一定的选择性。这些类似物中最有效的化合物19，在ERα上的K(i)=20nM。这些分子代表了一种用于设计潜在有用的雌激素受体配体的新型模板。
