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Updated: Aug 2, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor
B R Henke1, D H Drewry, S A Jones
1Department of Medicinal Chemistry, Glaxo Wellcome Research and Development, Five Moore Drive, 27709, Research Triangle Park, NC, USA. brh14990@gsk.com
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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