Synthesis and evaluation of 18F-labeled 4-nitrobenzyl derivatives for imaging tumor hypoxia with positron emission tomography: Comparison of 2-[18F]fluoroethyl carbonate and 2-[18F]fluoroethyl carbamate

被引：3
作者：
Zhang, Zhengxing [1 ]
Lau, Joseph [1 ]
Kuo, Hsiou-Ting [1 ]
Zhang, Chengcheng [1 ]
Hundal-Jabal, Navjit [1 ]
Colpo, Nadine [1 ]
Benard, Francois [1 ,2 ]
Lin, Kuo-Shyan [1 ,2 ]
机构：
[1] British Columbia Canc Res Ctr, Dept Mol Oncol, Vancouver, BC V5Z 1L3, Canada
[2] Univ British Columbia, Dept Radiol, Vancouver, BC V5Z 4E3, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 02期
基金：
加拿大健康研究院;
关键词：
Hypoxia; Positron emission tomography; Fluorine-18; Nitroreductase; 2-Fluoroethanol; 2-Fluoroethylamine; PRODRUG THERAPY; DIRECTED ENZYME; PET; OXYGENATION; HEAD; F-18-FLUOROMISONIDAZOLE; BIODISTRIBUTION; ACTIVATION; RESISTANCE; INHIBITORS;
D O I：
10.1016/j.bmcl.2015.11.066
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two 4-nitrobenzyl derivatives, 2-fluoroethyl 4-nitrobenzyl carbonate 1 and 4-nitrobenzyl N-2-fluoroethyl carbamate 2, were radiolabeled with F-18 and evaluated for imaging tumor hypoxia with positron emission tomography. Although good tumor uptake was observed for [F-18] 1 and [F-18] 2 (>2.5% ID/g at 3-h post-injection), the tracers cleared slowly from nontarget tissues (>1.5% ID/g) and exhibited extensive defluorination in vivo (>4.0% ID/g for bone). Therefore, [F-18] 1 and [F-18] 2 are not suitable for imaging tumor hypoxia due to suboptimal tumor-to-background contrasts. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码：584 / 588
页数：5
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