Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Bioorg Med Chem Lett. 2020 Nov 15;30(22):127582. doi: 10.1016/j.bmcl.2020.127582. Epub 2020 Sep 28.
A 4-nitroimidazole xanthate ligand (NMXT) was synthesized and radiolabeled with [TcN] core and [TcO] core to obtain TcN-NMXT and TcO-NMXT, respectively. The two Tc-complexes were prepared with high radiochemical purity and had good stability. The partition coefficient results indicated both of them were hydrophilic, and cellular uptake studies showed they exhibited good hypoxic selectivity. From the biodistribution study results, TcO-NMXT showed more favourable tumor uptake (1.73 ± 0.14 ID%/g) and higher tumor/muscle ratio (7.01 ± 0.16) than TcN-NMXT at 4 h post-injection. Single photon emission computed tomography (SPECT) imaging study of TcO-NMXT showed there was a visible accumulation in tumor site, suggesting it would be a promising candidate as a tumor hypoxia imaging agent.
合成了一种 4-硝基咪唑黄原酸配体（NMXT），并用 [TcN] 核和 [TcO] 核标记，分别得到 TcN-NMXT 和 TcO-NMXT。这两种 Tc 配合物均具有高放射化学纯度和良好的稳定性。分配系数结果表明它们均具有亲水性，细胞摄取研究表明它们具有良好的低氧选择性。从生物分布研究结果来看，TcO-NMXT 在注射后 4 小时表现出更高的肿瘤摄取（1.73±0.14 ID%/g）和更高的肿瘤/肌肉比（7.01±0.16）。TcO-NMXT 的单光子发射计算机断层扫描（SPECT）成像研究表明，肿瘤部位有明显的聚集，表明它可能成为一种有前途的肿瘤缺氧成像剂。
