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Synthesis, Radiosynthesis, and in vitro Studies on Novel Hypoxia PET Tracers Incorporating [18F]FDR
European Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2021-02-09 , DOI: 10.1002/ejoc.202001670
Matteo Zanda 1 , Manuele Musolino 2 , Ian N. Fleming 2 , Lutz F. Schweiger 2 , David O’Hagan 3 , Sergio Dall’Angelo 2
Affiliation  

The synthesis of five radiotracers incorporating different oxyamine spacers between the hypoxia‐reactive 2‐nitroimidazole moiety and the [18F]FDR (2‐fluorodeoxyribose) prosthetic group is described. The lead compound – carrying a cyclopropyl spacer – displayed superior uptake kinetics and similar selectivity for hypoxic cells relative to the gold standard hypoxia tracers [18F]FAZA and [18F]FMISO.
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中文翻译:

新型[18F] FDR的低氧PET示踪剂的合成,放射合成和体外研究

描述了五种放射性示踪剂的合成,这些放射性示踪剂在缺氧反应性2-硝基咪唑部分与[ 18 F] FDR(2-氟脱氧核糖)修复基团之间掺入了不同的羟胺间隔基。相对于金标准缺氧示踪剂[ 18 F] FAZA和[ 18 F] FMISO,带有环丙基间隔基的先导化合物对缺氧细胞显示出优异的吸收动力学和相似的选择性。
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更新日期:2021-03-01
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