Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines.
A series of nonsteroidal human androgen receptor (hAR) antagonists based on 8-substituted 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethylpyrido[3,2-g]quin olines was synthesized. Compounds in this series were tested for the ability to bind to hAR and inhibit hAR-dependent transcription in a mammalian cellular background.
Kong
J W
JW
Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
Hamann
L G
LG
Ruppar
D A
DA
Edwards
J P
JP
Marschke
K B
KB
Jones
T K
TK
D000726:Androgen Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D059002:Androgen Receptor Antagonists; D000728:Androgens / Q000378:metabolism; D000818:Animals; D019556:COS Cells; D006801:Humans; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D014158:Transcription, Genetic / Q000187:drug effects
D000726:Androgen Antagonists; D059002:Androgen Receptor Antagonists; D000728:Androgens; D011728:Pyridones; D011804:Quinolines