Li Zejun, Chu Taiwei, Liu Xinqi, Wang Xiangyun
Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Nucl Med Biol. 2005 Apr;32(3):225-31. doi: 10.1016/j.nucmedbio.2005.01.004.
Three novel nitroimidazole-based thioflavin-T derivatives, N-[4-(benzothiazol-2-yl)phenyl]-3-(4-nitroimidazole-1-yl)propanamide, N-[4-(benzothiazol-2-yl) phenyl]-3-(4-nitroimidazole-1-yl)-N-methylpropanamide and N-[4-(benzothiazol-2-yl)phenyl]-3-(2-nitroimidazole-1-yl) propanamide were synthesized and radiolabeled with iodine-131. Three (131)I-labeled compounds continuously accumulated in hypoxic murine sarcoma S180 cells in vitro but not in aerobic cells. Biodistribution results in mice bearing S180 tumor indicated that the tracers could localize in the tumor and eliminate from it slowly. In contrast, the uptake in other organs (stomach excluded) was little and the clearance was quick. The tumor-to-tissue ratios of three compounds all increased with time.
合成了三种新型的基于硝基咪唑的硫黄素 - T衍生物，即N - [4 -（苯并噻唑 - 2 - 基）苯基] - 3 -（4 - 硝基咪唑 - 1 - 基）丙酰胺、N - [4 -（苯并噻唑 - 2 - 基）苯基] - 3 -（4 - 硝基咪唑 - 1 - 基）- N - 甲基丙酰胺和N - [4 -（苯并噻唑 - 2 - 基）苯基] - 3 -（2 - 硝基咪唑 - 1 - 基）丙酰胺，并用碘 - 131进行了放射性标记。三种131I标记的化合物在体外能持续积聚在缺氧的小鼠肉瘤S180细胞中，但在有氧细胞中则不会。对荷S180肿瘤小鼠的生物分布研究结果表明，这些示踪剂能够在肿瘤中定位并缓慢从肿瘤中清除。相比之下，在其他器官（不包括胃）中的摄取量很少且清除速度很快。三种化合物的肿瘤与组织比值均随时间增加。
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