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Synthesis and evaluation of novel F-18 labeled fluoroarylvaline derivatives: Potential PET imaging agents for tumor detection

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机构: [a]Key laboratory of Radiopharmaceuticals, College of Chemistry, Beijing Normal University, Beijing 100875, People’s Republic of China [b]Center of PET, Xuan Wu Hospital, Beijing 100053, People’s Republic of China
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关键词: Amino acids F-18 labeled Fluoroarylvaline derivatives PET imaging agents Tumor detection

摘要:
Two F-18 labeled fluoroarylvaline derivatives, methyl 2-(2-[F-18]fluoro-4-nitrobenzamido)-3-methylbutanoate ([F-18]1, [F-18]MFNBMB) and its corresponding acid 2-(2-[F-18]fluoro-4-nitrobenzamido)-3-methylbutanoic acid ([F-18]2, [F-18]FNBMBA), have been designed and synthesized, respectively, by our team. Meanwhile, we research on their biodistributions in mice model bearing S 180 tumor. Furthermore, we also carried out the biological evaluations of 2-[F-18]fluorodeoxyglucose ([F-18]FDG) and O-2-[18F]fluoroethyl- L-tyrosine (L-[18F]FET) in the same model for comparison with our targeting molecules [F-18]1 and [F-18]2. Excitingly, the tumor/blood (T/Bl) and tumor/brain (T/Br) ratios were 2.91, 7.06 at 30 min, 3.44, 5.61 at 60 min post injection for [F-18]1, 2.32, 13.30 for [F-18]2 at 30 min post injection, which were obviously superior to [F-18] FDG and L-[F-18] FET in the same model and demonstrated that [F-18]1 and [F-18]2, especially [F-18]2, were potential PET imaging agents for tumor detection. (C) 2009 Elsevier Ltd. All rights reserved.

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出版当年[2008]版:
大类 | 3 区 医学
小类 | 3 区 药物化学 3 区 有机化学
最新[2023]版:
大类 | 4 区 医学
小类 | 2 区 有机化学 4 区 药物化学
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出版当年[2007]版:
Q2 CHEMISTRY, ORGANIC Q2 CHEMISTRY, MEDICINAL
最新[2023]版:
Q2 CHEMISTRY, ORGANIC Q3 CHEMISTRY, MEDICINAL

影响因子: 最新[2023版] 最新五年平均 出版当年[2007版] 出版当年五年平均 出版前一年[2006版] 出版后一年[2008版]

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第一作者机构: [a]Key laboratory of Radiopharmaceuticals, College of Chemistry, Beijing Normal University, Beijing 100875, People’s Republic of China
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通讯机构: [a]Key laboratory of Radiopharmaceuticals, College of Chemistry, Beijing Normal University, Beijing 100875, People’s Republic of China
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