Author/Authors :
Arjan van Oeveren، نويسنده , , Mehrnoush Motamedi، نويسنده , , Esther Martinborough، نويسنده , , Shuo Zhao، نويسنده , , Yixing Shen، نويسنده , , Sarah West، نويسنده , , William Chang، نويسنده , , E. Adam Kallel، نويسنده , , Keith B. Marschke، نويسنده , , Francisco J. Lopez، نويسنده , , Andrés Negro-Vilar، نويسنده , , Lin Zhi، نويسنده ,
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.
Keywords :
AR agonist , androgen receptor , SARM , 2-Quinolinone
