title: 4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.
abstract: A series of human androgen receptor (hAR) agonists based on 4-alkyl-; 4,4-dialkyl-; and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinoline was synthesized and evaluated in competitive receptor binding assays and an androgen receptor cotransfection assay in a mammalian cell background. A number of compounds in this series demonstrated activity equal to or better than dihydrotestosterone in both assays and represent a novel class of compounds for use in androgen replacement therapy.
authors.affiliation: Department of Medicinal Chemistry, Ligand Pharmaceuticals, Inc., San Diego, CA 92121, USA.
authors.forename: R I
authors.initials: RI
authors.lastname: Higuchi
authors.forename: J P
authors.initials: JP
authors.lastname: Edwards
authors.forename: T R
authors.initials: TR
authors.lastname: Caferro
authors.forename: J D
authors.initials: JD
authors.lastname: Ringgenberg
authors.forename: J W
authors.initials: JW
authors.lastname: Kong
authors.forename: L G
authors.initials: LG
authors.lastname: Hamann
authors.forename: K L
authors.initials: KL
authors.lastname: Arienti
authors.forename: K B
authors.initials: KB
authors.lastname: Marschke
authors.forename: R L
authors.initials: RL
authors.lastname: Davis
authors.forename: L J
authors.initials: LJ
authors.lastname: Farmer
authors.forename: T K
authors.initials: TK
authors.lastname: Jones
mesh_terms: D000728:Androgens; D000818:Animals; D019556:COS Cells; D013196:Dihydrotestosterone / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D011485:Protein Binding; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000728:Androgens; D015363:Quinolones; D013196:Dihydrotestosterone