2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor. |
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| Authors: | B R Henke D H Drewry S A Jones E L Stewart S L Weaver R W Wiethe |
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| Institution: | Department of Medicinal Chemistry, Glaxo Wellcome Research and Development, Five Moore Drive, 27709, Research Triangle Park, NC, USA. brh14990@gsk.com |
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| Abstract: | 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. |
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