title: 2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.
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.
authors.affiliation: Department of Medicinal Chemistry, Glaxo Wellcome Research and Development, Five Moore Drive, 27709, Research Triangle Park, NC, USA. brh14990@gsk.com
authors.forename: B R
authors.initials: BR
authors.lastname: Henke
authors.forename: D H
authors.initials: DH
authors.lastname: Drewry
authors.forename: S A
authors.initials: SA
authors.lastname: Jones
authors.forename: E L
authors.initials: EL
authors.lastname: Stewart
authors.forename: S L
authors.initials: SL
authors.lastname: Weaver
authors.forename: R W
authors.initials: RW
authors.lastname: Wiethe
mesh_terms: D001419:Bacteria / Q000235:genetics / Q000378:metabolism; D001665:Binding Sites / Q000502:physiology; D018360:Crystallography, X-Ray; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D006801:Humans; D008024:Ligands; D011485:Protein Binding / Q000502:physiology; D011725:Pyridines / Q000138:chemical synthesis / Q000378:metabolism; D020849:Raloxifene Hydrochloride / Q000378:metabolism; D011960:Receptors, Estrogen / Q000378:metabolism*; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology*; D012680:Sensitivity and Specificity
chemical_list: D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D008024:Ligands; D011725:Pyridines; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; D020849:Raloxifene Hydrochloride