Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, People's Republic of China.
Mol Pharm. 2021 Mar 1;18(3):1356-1363. doi: 10.1021/acs.molpharmaceut.0c01177. Epub 2021 Feb 15.
A novel glucose derivative (CN7DG) possessing an isonitrile as a coordinating group was synthesized, and Tc-CN7DG, which was expected to be a powerful tumor imaging agent for SPECT, was prepared in a kit by the reaction of CN7DG with SnCl·2HO and TcO. Tc-CN7DG exhibited good stability and was transported via glucose transporters. Biodistribution results in mice bearing A549 tumor models showed that Tc-CN7DG had a higher uptake at the tumor sites and better tumor/blood and tumor/muscle ratios than did [F]FDG and Tc-CN5DG. SPECT/CT imaging studies showed obvious accumulation in tumor sites, suggesting that Tc-CN7DG is a promising candidate for tumor imaging. Because Tc and Re stand for a "theranostic pair", Re-CN7DG is expected to be prepared as a promising agent for tumor therapy.
一种新型葡萄糖衍生物（CN7DG）被合成出来，它具有一个作为配位基团的异腈。预计 Tc-CN7DG 将成为 SPECT 的一种强大的肿瘤成像剂，它是通过 CN7DG 与 SnCl·2HO 和 TcO 的反应在试剂盒中制备的。Tc-CN7DG 表现出良好的稳定性，并通过葡萄糖转运体进行运输。在携带 A549 肿瘤模型的小鼠中的生物分布结果表明，与 [F]FDG 和 Tc-CN5DG 相比，Tc-CN7DG 在肿瘤部位有更高的摄取率，并且具有更好的肿瘤/血液和肿瘤/肌肉比值。SPECT/CT 成像研究表明在肿瘤部位有明显的聚集，表明 Tc-CN7DG 是一种有前途的肿瘤成像候选物。因为 Tc 和 Re 代表了“治疗诊断对”，所以预计 Re-CN7DG 将被制备为一种有前途的肿瘤治疗剂。
