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

Authors
Van Dort, ME Jung, YW
Citation
Me. Van Dort et Yw. Jung, Synthesis and structure-activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands, BIOORG MED, 11(8), 2001, pp. 1045-1047
Citations number
20
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
8
Year of publication
2001
Pages
1045 - 1047
Database
ISI
SICI code
0960-894X(20010423)11:8<1045:SASSOS>2.0.ZU;2-X
Abstract
A series of arylhydantoin derivatives modeled after the antiandrogen RU 588 41 was generated to identify potential candidates for development as androg en receptor (AR) radioligands. Side-chain modified derivatives of RU 58841, suitable for labeling with either carbon-ii or radiohalogens (flourine-18 iodine-123), were synthesized and tested for their AR binding affinities. T he N-(iodopropenyl) derivative 13 (K-i = 13nM) is a potential candidate for development as a radioiodinated AR ligand. (C) 2001 Elsevier Science Ltd. All rights reserved.