Title of article
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
1527
To page
1531
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797880
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