Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
A series of alkylamino-2-quinolinone compounds (3) was discovered as androgen receptor modulators based on an early linear tricyclic quinoline pharmacophore (1). The series demonstrated selective high binding affinity to androgen receptor and potent receptor modulating activities in the cotransfection assays.
van Oeveren
Arjan
A
Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA.
Pio
Barbara A
BA
Tegley
Christopher M
CM
Higuchi
Robert I
RI
Wu
Min
M
Jones
Todd K
TK
Marschke
Keith B
KB
Negro-Vilar
Andrés
A
Zhi
Lin
L
D000726:Androgen Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D059002:Androgen Receptor Antagonists; D000728:Androgens; D000813:Anilides / Q000494:pharmacology; D000818:Animals; D002460:Cell Line; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D009570:Nitriles / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011944:Receptors, Androgen / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014105:Tosyl Compounds / Q000494:pharmacology; D014162:Transfection
D000726:Androgen Antagonists; D059002:Androgen Receptor Antagonists; D000728:Androgens; D000813:Anilides; D007202:Indicators and Reagents; D009570:Nitriles; D011804:Quinolines; D011944:Receptors, Androgen; D014105:Tosyl Compounds; C053541:bicalutamide