title: Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
abstract: A series of ligands with varying heterocyclic cores and substituents that display a range of selectivity's (up to >100x) for ER-beta over ER-alpha are reported.
authors.affiliation: Cardiovascular and Metabolic Diseases, Medicinal Chemistry, Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. rchesworth@gmail.com
authors.forename: Richard
authors.initials: R
authors.lastname: Chesworth
authors.forename: Matthew D
authors.initials: MD
authors.lastname: Wessel
authors.forename: Lisa
authors.initials: L
authors.lastname: Heyden
authors.forename: F Michael
authors.initials: FM
authors.lastname: Mangano
authors.forename: Michael
authors.initials: M
authors.lastname: Zawistoski
authors.forename: Laura
authors.initials: L
authors.lastname: Gegnas
authors.forename: David
authors.initials: D
authors.lastname: Galluzzo
authors.forename: Bruce
authors.initials: B
authors.lastname: Lefker
authors.forename: Kimberly O
authors.initials: KO
authors.lastname: Cameron
authors.forename: Jeanne
authors.initials: J
authors.lastname: Tickner
authors.forename: Bihong
authors.initials: B
authors.lastname: Lu
authors.forename: Tessa A
authors.initials: TA
authors.lastname: Castleberry
authors.forename: Donna N
authors.initials: DN
authors.lastname: Petersen
authors.forename: Amy
authors.initials: A
authors.lastname: Brault
authors.forename: Pia
authors.initials: P
authors.lastname: Perry
authors.forename: Oicheng
authors.initials: O
authors.lastname: Ng
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Owen
authors.forename: Lydia
authors.initials: L
authors.lastname: Pan
authors.forename: Hua-Zhu
authors.initials: HZ
authors.lastname: Ke
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Brown
authors.forename: David D
authors.initials: DD
authors.lastname: Thompson
authors.forename: Paul
authors.initials: P
authors.lastname: DaSilva-Jardine
mesh_terms: D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D047628:Estrogen Receptor alpha / Q000378:metabolism; D047629:Estrogen Receptor beta / Q000737:chemistry / Q000378:metabolism*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D008024:Ligands; D020845:Selective Estrogen Receptor Modulators / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D008024:Ligands; D020845:Selective Estrogen Receptor Modulators