Medicinal Inorganic Chemistry Group, Department of Chemistry, The University of British Columbia, 2036 Main Mall, Vancouver, BC, V6T 1Z1, Canada.
Dalton Trans. 2009 Nov 14(42):9216-27. doi: 10.1039/b914310f. Epub 2009 Sep 25.
The design rationale, synthesis and radiolabeling evaluation of four glucosamine conjugated ligands for the (99m)Tc(CO)(3) core is described. The capability to bind the tricarbonyl core is initially demonstrated using the cold surrogate Re(CO)(3). The four compounds are competent chelates in binding (99m)Tc(CO)(3) as labeling studies show, with yields ranging from 79 to 96% and the resulting complexes showing stability in the presence of competing chelates for 24 h at 37 degrees C. The rhenium complexes were tested for hexokinase-catalysed phosphorylation, and the technetium complexes were tested for GLUT-1 mediated cell uptake--they showed a small amount of uptake but it was not glucose dependent, suggesting that it was not via the GLUT-1 transporters.
描述了四种用于 (99m)Tc(CO)(3) 核心的葡糖胺缀合配体的设计原理、合成和放射性标记评估。最初使用冷替代物 Re(CO)(3) 证明了结合三羰基核心的能力。四项化合物作为标记研究表明，作为配合物在结合 (99m)Tc(CO)(3) 方面具有竞争力，产率范围为 79% 至 96%，并且在 37°C 下 24 小时内存在竞争配合物时，所得配合物稳定。对铼配合物进行了己糖激酶催化磷酸化测试，对锝配合物进行了 GLUT-1 介导的细胞摄取测试 - 它们显示出少量摄取，但不是葡萄糖依赖性的，这表明不是通过 GLUT-1 转运蛋白。
