Title of article :
Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity
Author/Authors :
Yun Oliver Long، نويسنده , , Robert I. Higuchi، نويسنده , , Thomas R. Caferro، نويسنده , , Thomas L.S. Lau، نويسنده , , Min Wu، نويسنده , , Marquis L. Cummings، نويسنده , , Esther A. Martinborough، نويسنده , , Keith B. Marschke، نويسنده , , William Y. Chang، نويسنده , , Francisco J. Lopez، نويسنده , , Donald S. Karanewsky، نويسنده , , Lin Zhi، نويسنده ,
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 , Androgenic , Benzoxazine , AR , muscle , Anabolic , 2-g]quinolin-7-one