Design and synthesis of an array of selective androgen receptor modulators

Ryan P. Trump, Jean-Baptiste E. Blanc, Eugene L. Stewart, Peter J. Brown, Matilde Caivano, David W. Gray, William J. Hoekstra, Timothy M. Willson, Bajin Han, Philip Turnbull

    Research output: Contribution to journalArticlepeer-review

    19 Citations (Scopus)

    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.
    Original languageEnglish
    Pages (from-to)107-14
    Number of pages8
    JournalJournal of Combinatorial Chemistry
    Volume9
    Issue number1
    DOIs
    Publication statusPublished - 2007

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