2. Academic Validation
  3. Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity

Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity

  • Bioorg Med Chem Lett. 2008 May 1;18(9):2967-71. doi: 10.1016/j.bmcl.2008.03.062.
Yun Oliver Long 1,  Robert I Higuchi,  Thomas R Caferro,  Thomas L S Lau,  Min Wu,  Marquis L Cummings,  Esther A Martinborough,  Keith B Marschke,  William Y Chang,  Francisco J López,  Donald S Karanewsky,  Lin Zhi
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA.
PMID: 18400499 DOI: 10.1016/j.bmcl.2008.03.062
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.

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