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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Androgen Antagonists / chemical synthesis*
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Androgen Antagonists / metabolism
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Androgen Antagonists / pharmacology*
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Animals
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Binding Sites / physiology
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Carbon Isotopes / chemistry
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Fluorine / chemistry
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Hydantoins / chemical synthesis
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Hydantoins / metabolism
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Imidazoles / chemical synthesis*
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Imidazoles / metabolism
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Imidazoles / pharmacology*
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Nitriles / chemical synthesis*
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Nitriles / metabolism
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Nitriles / pharmacology*
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Radioligand Assay
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Rats
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Receptors, Androgen / metabolism*
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Structure-Activity Relationship
Substances
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4-(4,4-dimethyl-2,5-dioxo-3-N-(iodopropenyl)-1-imidazolidinyl)-2- (trifluoromethyl)benzonitrile
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Androgen Antagonists
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Carbon Isotopes
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Hydantoins
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Imidazoles
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Nitriles
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Receptors, Androgen
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RU 58841
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Fluorine