Title of article :
4-Alkyl- and 3,4-dialkyl-1,2,3,4,-tetrahydro-8-pyridono[5,6-g]quinolines: Potent, nonsteroidal androgen receptor agonists
Author/Authors :
Robert I. Higuchi، نويسنده , , James P. Edwards، نويسنده , , Thomas R. Caferro، نويسنده , , Josef D. Ringgenberg، نويسنده , , James W. Kong، نويسنده , , Lawrence G. Hamann، نويسنده , , Kristen L. Arienti، نويسنده , , Keith B. Marschke، نويسنده , , Robert L. Davis، نويسنده , , Luc J. Farmer، نويسنده , , Todd K. Jones، نويسنده ,
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.
