title: Diaryl-substituted salicyl- and anthranyl-ketoximes as potential estrogen receptor ligands.
abstract: 3,4-diphenylsalicylaldoxime and 3,4-diphenylanthranylaldoxime derivatives, containing small groups (methyl or ethyl) on the imine carbon atom, were synthesized and submitted to biological assays. Binding tests performed on uterine cytosol estrogen receptor (ER) preparation and on purified full-length human ERalpha and ERbeta, showed that the newly synthesised compounds exhibit considerably lower binding affinities with respect to reference non-substituted 3,4-salicylaldoxime.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
authors.forename: Filippo
authors.initials: F
authors.lastname: Minutolo
authors.forename: Michela
authors.initials: M
authors.lastname: Antonello
authors.forename: Simone
authors.initials: S
authors.lastname: Bertini
authors.forename: Giorgio
authors.initials: G
authors.lastname: Placanica
authors.forename: Simona
authors.initials: S
authors.lastname: Rapposelli
authors.forename: Kathryn E
authors.initials: KE
authors.lastname: Carlson
authors.forename: John A
authors.initials: JA
authors.lastname: Katzenellenbogen
authors.forename: Marco
authors.initials: M
authors.lastname: Macchia
mesh_terms: D001667:Binding, Competitive / Q000187:drug effects; D047628:Estrogen Receptor alpha / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism; D047629:Estrogen Receptor beta / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D010091:Oximes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011960:Receptors, Estrogen / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D008024:Ligands; D010091:Oximes; D011960:Receptors, Estrogen