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Merck
  • Synthesis and structure-activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands.

Synthesis and structure-activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands.

Bioorganic & medicinal chemistry letters (2001-05-01)
M E Van Dort, Y W Jung
摘要

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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4-碘溴苄, 95%