title: Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
abstract: Modification on a lead series of [1,4]oxazino[3,2-g]quinolin-7-ones at the 2-position led to selective androgen receptor modulators with improved in vivo activity. The most potent analog (-)-33a exhibited full maintenance of levator ani muscle at 3mg/kg and reduced activity on ventral prostate weight in a 2-week orally-dosed and orchidectomized rat maintenance assay.
authors.affiliation: Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA.
authors.forename: Yun Oliver
authors.initials: YO
authors.lastname: Long
authors.forename: Robert I
authors.initials: RI
authors.lastname: Higuchi
authors.forename: Thomas R
authors.initials: TR
authors.lastname: Caferro
authors.forename: Thomas L S
authors.initials: TL
authors.lastname: Lau
authors.forename: Min
authors.initials: M
authors.lastname: Wu
authors.forename: Marquis L
authors.initials: ML
authors.lastname: Cummings
authors.forename: Esther A
authors.initials: EA
authors.lastname: Martinborough
authors.forename: Keith B
authors.initials: KB
authors.lastname: Marschke
authors.forename: William Y
authors.initials: WY
authors.lastname: Chang
authors.forename: Francisco J
authors.initials: FJ
authors.lastname: López
authors.forename: Donald S
authors.initials: DS
authors.lastname: Karanewsky
authors.forename: Lin
authors.initials: L
authors.lastname: Zhi
mesh_terms: D000284:Administration, Oral; D045930:Anabolic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D059002:Androgen Receptor Antagonists; D000728:Androgens; D000818:Animals; D008297:Male; D008956:Models, Chemical; D009919:Orchiectomy; D009929:Organ Size / Q000187:drug effects; D010078:Oxazines / Q000138:chemical synthesis / Q000494:pharmacology*; D011467:Prostate / Q000033:anatomy & histology / Q000187:drug effects*; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011944:Receptors, Androgen; D013329:Structure-Activity Relationship; D013739:Testosterone / Q000494:pharmacology
chemical_list: D045930:Anabolic Agents; D059002:Androgen Receptor Antagonists; D000728:Androgens; D010078:Oxazines; D015363:Quinolones; D011944:Receptors, Androgen; D013739:Testosterone