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Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity
Authors:Long Yun Oliver  Higuchi Robert I  Caferro Thomas R  Lau Thomas L S  Wu Min  Cummings Marquis L  Martinborough Esther A  Marschke Keith B  Chang William Y  López Francisco J  Karanewsky Donald S  Zhi Lin
Affiliation:

aDiscovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA

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 3 mg/kg and reduced activity on ventral prostate weight in a 2-week orally-dosed and orchidectomized rat maintenance assay.
Keywords:Androgen   SARM   Testosterone   Anabolic   Androgenic   Benzoxazine   AR   Muscle   Oxazino[3,2-g]quinolin-7-one
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