title: 7-Substituted 2-phenyl-benzofurans as ER beta selective ligands.
abstract: A series of 2-(4-hydroxy-phenyl)-benzofuran-5-ols with relatively lipophilic groups in the 7-position of the benzofuran was prepared and the affinity and selectivity for ER beta was measured. Many of the analogues were found to be potent and selective ER beta ligands. Additional modifications at the benzofuran 4-position as well as at the 3'-position of the 2-phenyl group were found to further increase selectivity. Such modifications led to compounds with <10 nM potency and >100-fold selectivity for ER beta.
authors.affiliation: Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. collinm2@wyeth.com
authors.forename: Michael D
authors.initials: MD
authors.lastname: Collini
authors.forename: David H
authors.initials: DH
authors.lastname: Kaufman
authors.forename: Eric S
authors.initials: ES
authors.lastname: Manas
authors.forename: Heather A
authors.initials: HA
authors.lastname: Harris
authors.forename: Ruth A
authors.initials: RA
authors.lastname: Henderson
authors.forename: Zhang B
authors.initials: ZB
authors.lastname: Xu
authors.forename: Rayomand J
authors.initials: RJ
authors.lastname: Unwalla
authors.forename: Chris P
authors.initials: CP
authors.lastname: Miller
mesh_terms: D001572:Benzofurans / Q000138:chemical synthesis* / Q000378:metabolism; D045744:Cell Line, Tumor; D047629:Estrogen Receptor beta / Q000819:agonists* / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D018974:Insulin-Like Growth Factor Binding Protein 4 / Q000235:genetics; D008024:Ligands; D012333:RNA, Messenger / Q000032:analysis; D013329:Structure-Activity Relationship
chemical_list: D001572:Benzofurans; D047629:Estrogen Receptor beta; D018974:Insulin-Like Growth Factor Binding Protein 4; D008024:Ligands; D012333:RNA, Messenger