Design and synthesis of an array of selective androgen receptor modulators |
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Authors: | Trump Ryan P Blanc Jean-Baptiste E Stewart Eugene L Brown Peter J Caivano Matilde Gray David W Hoekstra William J Willson Timothy M Han Bajin Turnbull Philip |
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Affiliation: | GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA. ryan.p.trump@gsk.com |
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Abstract: | We describe the design, using shape comparison and fast docking computer algorithms, and rapid parallel synthesis of a 1300 member array based on GSK7721, a 4-aminobenzonitrile androgen receptor (AR) antagonist identified by focused screening of the GSK compound collection. The array yielded 352 submicromolar and 17 subnanomolar AR agonists as measured by a cell-based reporter gene functional assay. The rapid synthesis of a large number of active compounds provided valuable information in the optimization of AR modulators, which may be useful in treating androgen deficiency in aging males. |
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