title: Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
abstract: A series of alkylamino-2-quinolinone compounds (3) was discovered as androgen receptor modulators based on an early linear tricyclic quinoline pharmacophore (1). The series demonstrated selective high binding affinity to androgen receptor and potent receptor modulating activities in the cotransfection assays.
authors.affiliation: Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA.
authors.forename: Arjan
authors.initials: A
authors.lastname: van Oeveren
authors.forename: Barbara A
authors.initials: BA
authors.lastname: Pio
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Tegley
authors.forename: Robert I
authors.initials: RI
authors.lastname: Higuchi
authors.forename: Min
authors.initials: M
authors.lastname: Wu
authors.forename: Todd K
authors.initials: TK
authors.lastname: Jones
authors.forename: Keith B
authors.initials: KB
authors.lastname: Marschke
authors.forename: Andrés
authors.initials: A
authors.lastname: Negro-Vilar
authors.forename: Lin
authors.initials: L
authors.lastname: Zhi
mesh_terms: D000726:Androgen Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D059002:Androgen Receptor Antagonists; D000728:Androgens; D000813:Anilides / Q000494:pharmacology; D000818:Animals; D002460:Cell Line; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D009570:Nitriles / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011944:Receptors, Androgen / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014105:Tosyl Compounds / Q000494:pharmacology; D014162:Transfection
chemical_list: D000726:Androgen Antagonists; D059002:Androgen Receptor Antagonists; D000728:Androgens; D000813:Anilides; D007202:Indicators and Reagents; D009570:Nitriles; D011804:Quinolines; D011944:Receptors, Androgen; D014105:Tosyl Compounds; C053541:bicalutamide