4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists

  • Bioorg Med Chem Lett. 1999 May 3;9(9):1335-40. doi: 10.1016/s0960-894x(99)00186-9.
R I Higuchi  1 ,  J P Edwards ,  T R Caferro ,  J D Ringgenberg ,  J W Kong ,  L G Hamann ,  K L Arienti ,  K B Marschke ,  R L Davis ,  L J Farmer ,  T K Jones
Affiliations
  • 1. Department of Medicinal Chemistry, Ligand Pharmaceuticals, Inc., San Diego, CA 92121, USA.
PMID: 10340624 DOI: 10.1016/s0960-894x(99)00186-9
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.