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Bioorg Med Chem Lett. 2001 Apr 23;11(8):1045-7.

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

Author information

1
Department of Radiology, The University of Michigan Medical School, Ann Arhor 48109-0552, USA. mvandort@umich.edu

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.

PMID:
11327585
DOI:
10.1016/s0960-894x(01)00146-9
[Indexed for MEDLINE]

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