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

B R Henke; D H Drewry; S A Jones; E L Stewart; S L Weaver; R W Wiethe

doi:10.1016/s0960-894x(01)00321-3

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

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1939-42. doi: 10.1016/s0960-894x(01)00321-3.

Authors

B R Henke¹, D H Drewry, S A Jones, E L Stewart, S L Weaver, R W Wiethe

Affiliation

¹ Department of Medicinal Chemistry, Glaxo Wellcome Research and Development, Five Moore Drive, 27709, Research Triangle Park, NC, USA. brh14990@gsk.com

PMID: 11459665
DOI: 10.1016/s0960-894x(01)00321-3

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.

MeSH terms

Bacteria / genetics
Bacteria / metabolism
Binding Sites / physiology
Crystallography, X-Ray
Estrogen Receptor alpha
Estrogen Receptor beta
Humans
Ligands
Protein Binding / physiology
Pyridines / chemical synthesis
Pyridines / metabolism
Raloxifene Hydrochloride / metabolism
Receptors, Estrogen / metabolism*
Selective Estrogen Receptor Modulators / chemical synthesis*
Selective Estrogen Receptor Modulators / pharmacology*
Sensitivity and Specificity

Substances

Estrogen Receptor alpha
Estrogen Receptor beta
Ligands
Pyridines
Receptors, Estrogen
Selective Estrogen Receptor Modulators
Raloxifene Hydrochloride