2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor

We have prepared a novel series of 2-amino-4,6-diarylpyridines that functio n as ligands of estrogen receptor alpha (ER alpha) and estrogen receptor be ta (ER beta). These compounds bind to both ER alpha and ER beta with a mode st selectivity for the alpha subtype. The most potent of these analogues, c ompound 19, has a K-i = 20nM at ER alpha. These molecules represent a novel template for designing potentially useful ligands for the estrogen recepto r. (C) 2001 Elsevier Science Ltd. All rights reserved.