90914-95-7Relevant articles and documents
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones
van Oeveren, Arjan,Motamedi, Mehrnoush,Martinborough, Esther,Zhao, Shuo,Shen, Yixing,West, Sarah,Chang, William,Kallel, Adam,Marschke, Keith B.,Lopez, Francisco J.,Negro-Vilar, Andres,Zhi, Lin
, p. 1527 - 1531 (2007/10/03)
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.