Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Delhi, India.
Cancer Biother Radiopharm. 2010 Apr;25(2):245-50. doi: 10.1089/cbr.2009.0663.
The synthesis of eight ligands by using 2-amino benzimidazole with different mono/bis aldehydes is described herein. The final products were characterized by spectral techniques such as FT-IR, (1)H NMR, and EI-Mass. The structure-activity relationships of the benzimidazole derivatives are also reported. Studies on the complexation of the ligands with (99m)Tc were optimized by using stannous tartrate as reducing agent under various reaction conditions. The radiochemical stability was >or=95% for all the complexes, and they were to be stable for 12-14 hours in serum. Most of the ligands showed fast blood clearance. Biodistribution studies of the (99m)Tc complexes of these ligands showed no significant uptake in the brain or in the heart, and the clearance was mainly through the hepatobiliary system. Among the eight compounds evaluated for their antiproliferative activity in vitro, L(8) produced good activity against the cancer cell lines A549 and PC-3.
本文描述了通过 2-氨基苯并咪唑与不同的单/双醛合成了 8 种配体。最终产物通过光谱技术（如 FT-IR、（1）H NMR 和 EI-Mass）进行了表征。还报道了苯并咪唑衍生物的构效关系。通过使用酒石酸亚锡作为还原剂，在各种反应条件下优化了配体与（99m）Tc 的络合。所有配合物的放射化学稳定性均大于等于 95%，在血清中稳定 12-14 小时。大多数配体表现出快速的血液清除率。这些配体的（99m）Tc 配合物的生物分布研究表明，它们在大脑或心脏中没有明显的摄取，清除主要通过肝胆系统进行。在评估的 8 种化合物中，L（8）对 A549 和 PC-3 癌细胞系表现出良好的体外增殖活性。
