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Synthesis and 18F-radiolabeling of thymidine AMBF3 conjugates
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-04-23 , DOI: 10.1039/d0md00054j
Antonio A W L Wong 1 , Jerome Lozada 1 , Mathieu L Lepage 1 , Chengcheng Zhang 2 , Helen Merkens 2 , Jutta Zeisler 2 , Kuo-Shyan Lin 2 , François Bénard 2 , David M Perrin 1
Affiliation  

In pursuit of 18F-labeled nucleosides for positron emission tomography (PET) imaging, we report on the chemical and radiochemical synthesis of two thymidine (dT) analogs, dT-C5-AMBF3 and dT-N3-AMBF3, that are radiofluorinated by isotope exchange (IEX) and studied as PET imaging agents in mice with tumor xenografts. dT-C5-AMBF3 shows preferential, and tumor-specific, uptake over dT-N3-AMBF3. This work provides a new synthetic method in order to access new nucleoside tracers for PET imaging.

中文翻译:


胸苷 AMBF3 缀合物的合成和 18F-放射性标记



为了寻找用于正电子发射断层扫描 (PET) 成像的18 F 标记核苷,我们报告了两种胸苷 (dT) 类似物 dT-C 5 -AMBF 3和 dT-N 3 -AMBF 3的化学和放射化学合成,通过同位素交换 (IEX) 进行放射性氟化,并在肿瘤异种移植小鼠中作为 PET 成像剂进行研究。 dT-C 5 -AMBF 3显示出优于 dT-N 3 -AMBF 3的优先且肿瘤特异性的摄取。这项工作提供了一种新的合成方法,以便获得用于 PET 成像的新核苷示踪剂。
更新日期:2020-04-23
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