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Bioorg Med Chem Lett. 2008 May 1;18(9):2967-71. doi: 10.1016/j.bmcl.2008.03.062. Epub 2008 Mar 23.

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

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1
Discovery 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 3mg/kg and reduced activity on ventral prostate weight in a 2-week orally-dosed and orchidectomized rat maintenance assay.

PMID:
18400499
DOI:
10.1016/j.bmcl.2008.03.062
[Indexed for MEDLINE]
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