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  • Title: Synthesis and structure-activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands.
    Author: Van Dort ME, Jung YW.
    Journal: Bioorg Med Chem Lett; 2001 Apr 23; 11(8):1045-7. PubMed ID: 11327585.
    Abstract:
    A series of arylhydantoin derivatives modeled after the antiandrogen RU 58841 was generated to identify potential candidates for development as androgen receptor (AR) radioligands. Side-chain modified derivatives of RU 58841, suitable for labeling with either carbon-11 or radiohalogens (fluorine-18, iodine-123), were synthesized and tested for their AR binding affinities. The N-(iodopropenyl) derivative 13 (Ki = 13 nM) is a potential candidate for development as a radioiodinated AR ligand.
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