A series of human androgen receptor (hAR) agonists based on 4-alkyl-: 4,4-d
ialkyl-; and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono [5,6-g] quinoline wa
s synthesized and evaluated In competitive receptor binding assays and an a
ndrogen receptor cotransfection assay in a mammalian cell background. A num
ber of compounds in this series demonstrated activity equal to or better th
an dihydrotestosterone in both assays and represent a novel class of compou
nds for use in androgen replacement therapy. (C) 1999 Elsevier Science Ltd.
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