title: Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators.
abstract: A library of benzofurans was prepared by solid-phase synthesis methods, and several analogues were identified as potent ligands for the estrogen receptors ER-alpha and ER-beta, with some compounds having selectivity for ER-alpha. Analogues designed to more closely mimic Raloxifene were less effective. Certain benzofurans were effective in a bone pit assay, but were characterized as agonists in a MCF-7 breast tumor cell proliferation assay.
authors.affiliation: Department of Chemistry Research, Bayer Research Center, 400Morgan Lane, West Haven, CT 06516, USA.
authors.forename: Roger A
authors.initials: RA
authors.lastname: Smith
authors.forename: Jinshan
authors.initials: J
authors.lastname: Chen
authors.forename: Mary M
authors.initials: MM
authors.lastname: Mader
authors.forename: Ingo
authors.initials: I
authors.lastname: Muegge
authors.forename: Ulrike
authors.initials: U
authors.lastname: Moehler
authors.forename: Suresh
authors.initials: S
authors.lastname: Katti
authors.forename: Diana
authors.initials: D
authors.lastname: Marrero
authors.forename: William G
authors.initials: WG
authors.lastname: Stirtan
authors.forename: Daniel R
authors.initials: DR
authors.lastname: Weaver
authors.forename: Hong
authors.initials: H
authors.lastname: Xiao
authors.forename: William
authors.initials: W
authors.lastname: Carley
mesh_terms: D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D002460:Cell Line; D015195:Drug Design; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005260:Female; D006801:Humans; D008958:Models, Molecular; D020849:Raloxifene Hydrochloride / Q000494:pharmacology; D011960:Receptors, Estrogen / Q000187:drug effects; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D001572:Benzofurans; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; D020849:Raloxifene Hydrochloride