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

被引：15

作者：

Van Dort, ME ^{[1
]}

Jung, YW ^{[1
]}

机构：

[1] Univ Michigan, Sch Med, Dept Radiol, Div Nucl Med, Ann Arbor, MI 48109 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(01)00146-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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-ii or radiohalogens (flourine-18 iodine-123), were synthesized and tested for their AR binding affinities. The 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.

引用

页码：1045 / 1047

页数：3

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