Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones |
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| Authors: | van Oeveren Arjan Motamedi Mehrnoush Martinborough Esther Zhao Shuo Shen Yixing West Sarah Chang William Kallel Adam Marschke Keith B López Francisco J Negro-Vilar Andrés Zhi Lin |
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| Affiliation: | Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. |
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| 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. |
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