1.
Bioorg Med Chem Lett
; 17(6): 1527-31, 2007 Mar 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17267219
RESUMO
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.