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

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. (C) 1999 Elsevier Science Ltd. All rights reserved.