793668-39-0Relevant articles and documents
Synthesis and structure-activity investigation of iodinated arylhydantoins and arylthiohydantoins for development as androgen receptor radioligands
Van Dort, Marcian E.,Jung, Yong-Woon
, p. 5285 - 5288 (2007/10/03)
A series of side-chain derivatives of the arylhydantoin RU 58841 and the arylthiohydantoin RU 59063, wherein the aromatic trifluoromethyl was replaced with iodine, was synthesized for development as radioiodinated androgen receptor (AR) ligands. Compounds having N-(methyl) and N-(hydroxybutyl) side-chains displayed high AR binding affinity (0.71 nM i i = 20-59 nM) towards the rat AR. Side-chains containing bulky lipophilic groups such as, benzyl and phenylpropyl, were poorly tolerated (Ki > 219 nM). Superior AR binding affinities (0.71 nM i 11 nM) were displayed by arylhydantoins and arylthiohydantoin derivatives containing hydroxybutyl or methyl side-chains. The latter compounds are potential candidates for development as radioiodinated AR ligands.