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Bioorg Med Chem Lett. 2007 Mar 15;17(6):1527-31. Epub 2007 Jan 8.

Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.

Author information

1
Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA.

Abstract

A series of selective androgen receptor modulators (SARMs) with a wide spectrum of receptor modulating activities was developed based on optimization of the 4-substituted 6-bisalkylamino-2-quinolinones (3). Significance of the trifluoromethyl group on the side chains and its interactions with amino acid residues within the androgen receptor (AR) ligand binding domain are discussed. A representative analog (9) was tested orally in a rodent model of hypogonadism and demonstrated desirable tissue selectivity.

PMID:
17267219
DOI:
10.1016/j.bmcl.2007.01.001
[Indexed for MEDLINE]

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