The objective of the study was to prepare and evaluate a 18F-radiolabled tracer (Al18F-5), derivated from the antitumor agent 2-(4-aminophenyl)benzothiazole, as a PET probe for tumor imaging. Al18F-5 was successfully prepared with approx. 40% radiochemical yield in aqueous phase. In in vitro cell uptake experiments and competition assay, Al18F-5 displayed good tumor-binding ability and specificity in HeLa cells (24.7 ± 0.9% ID/106 cells, IC50 = 63.8 ± 13.6 nM) and MCF-7 cells (6.8 ± 0.3% ID/106 cells, IC50 = 331.1 ± 33.7 nM). The nonradioactive compound, Al19F-5, visibly marked HeLa cells and MCF-7 cells but did not stain HEB cells in florescent staining, which further indicated the tumor-binding ability of Al18F-5. In in vivo PET imaging, HeLa and MCF-7 tumors were clearly delineated by specific accumulation of Al18F-5 in model mice. In biodistribution study, Al18F-5 exhibited good tumor uptake (4.66 ± 0.13% ID/g and 3.69 ± 0.56% ID/g, respectively), moderate tumor-to-muscle ratio (3.38 and 2.48, respectively) at 1 h post injection, which were in a good consistency with the results of PET imaging. In conclusion, Al18F-5 might be developed as a candidate PET probe for tumor imaging, though additional optimizations are still needed to improve pharmacokinetics in vivo.

中文翻译：

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Al18F-NODA配合物2-（4-氨基苯基）苯并噻唑作为潜在的肿瘤显像剂的合成与评价。

该研究的目的是制备和评估一种源自18F放射性示踪剂（Al18F-5），该示踪剂源自抗肿瘤药2-（4-氨基苯基）苯并噻唑，作为用于肿瘤成像的PET探针。Al18F-5已成功制备出约 在水相中放射化学产率为40％。在体外细胞摄取实验和竞争测定中，Al18F-5在HeLa细胞（24.7±0.9％ID / 106细胞，IC50 = 63.8±13.6 nM）和MCF-7细胞（6.8±0.3）中显示出良好的肿瘤结合能力和特异性％ID / 106个细胞，IC50 = 331.1±33.7 nM）。非放射性化合物Al19F-5可见地标记了HeLa细胞和MCF-7细胞，但在荧光染色中并未染色HEB细胞，这进一步表明了Al18F-5的肿瘤结合能力。在体内PET成像中，Al18F-5在模型小鼠中的特异性蓄积清楚地描绘了HeLa和MCF-7肿瘤。在生物分布研究中，Al18F-5在注射后1 h表现出良好的肿瘤吸收（分别为4.66±0.13％ID / g和3.69±0.56％ID / g），中等的肿瘤与肌肉比（分别为3.38和2.48） ，与PET成像的结果具有很好的一致性。总之，Al18F-5可能会被开发为肿瘤成像的候选PET探针，尽管仍需要其他优化来改善体内的药代动力学。