ERbeta ligands. Part 1: the discovery of ERbeta selective ligands which embrace the 4-hydroxy-biphenyl template.
The synthesis and structure-activity relationships of a series of simple biphenyls is described. Optimization of the 4-hydroxy-biphenyl template led to compounds with ERbeta selectivity on the order of 20-70-fold.
Edsall
Richard J
RJ
Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. mewshar@wyeth.com
Harris
Heather A
HA
Manas
Eric S
ES
Mewshaw
Richard E
RE
D001713:Biphenyl Compounds / Q000737:chemistry* / Q000378:metabolism*; D047629:Estrogen Receptor beta; D019833:Genistein / Q000737:chemistry / Q000378:metabolism; D006900:Hydroxylation; D020128:Inhibitory Concentration 50; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D011487:Protein Conformation; D011960:Receptors, Estrogen / Q000737:chemistry* / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D001713:Biphenyl Compounds; D047629:Estrogen Receptor beta; D008024:Ligands; D011960:Receptors, Estrogen; D019833:Genistein