title: Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
abstract: The androgen receptor is a member of the extended family of nuclear receptors and is widely distributed throughout the body. Androgen therapy is used to compensate for low levels of the natural hormones testosterone (T) and dihydrotestosterone and consists of administration of T, prodrugs thereof, or synthetic androgens. However, currently available androgens have many drawbacks. We identified 6-dialkylamino-4-trifluoromethylquinolin-2(1H)-ones as orally available tissue-selective androgen receptor modulators.
authors.affiliation: Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, California 92121, USA. avanoeveren@ligand.com
authors.forename: Arjan
authors.initials: A
authors.lastname: van Oeveren
authors.forename: Mehrnouch
authors.initials: M
authors.lastname: Motamedi
authors.forename: Neelakandha S
authors.initials: NS
authors.lastname: Mani
authors.forename: Keith B
authors.initials: KB
authors.lastname: Marschke
authors.forename: Francisco J
authors.initials: FJ
authors.lastname: López
authors.forename: William T
authors.initials: WT
authors.lastname: Schrader
authors.forename: Andrés
authors.initials: A
authors.lastname: Negro-Vilar
authors.forename: Lin
authors.initials: L
authors.lastname: Zhi
mesh_terms: D000284:Administration, Oral; D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000728:Androgens / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008958:Models, Molecular; D009919:Orchiectomy; D009929:Organ Size; D017773:Pelvic Floor / Q000033:anatomy & histology; D011467:Prostate / Q000033:anatomy & histology / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D011944:Receptors, Androgen / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: C515129:6-N,N-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethylquinolin-2(1H)-one; D000634:Aminoquinolines; D000728:Androgens; D011804:Quinolines; D015363:Quinolones; D011944:Receptors, Androgen