Novel Tc-99m labelled complexes with 2-nitroimidazole isocyanide: design, synthesis and evaluation as potential tumor hypoxia imaging agents

作者：Ruan Qing; Zhang Xuran; Lin Xiao; Duan Xiaojiang; Zhang Junbo^*

来源：Medchemcomm, 2018, 9(6): 988-994.

DOI：10.1039/c8md00107c

Radiolabelled 2-nitroimidazoles have been used for imaging hypoxia. With the aim of developing novel Tc-99m radiotracers for imaging hypoxia, four novel 2-nitroimidazole isocyanide derivatives (2a, 2b, 2c, and 2d) were synthesized and radiolabelling was carried out for preparing their corresponding Tc-99m complexes. These Tc-99m complexes were stable in vitro and could exhibit good hypoxic selectivity. The partition coefficient results indicated that they were hydrophilic, and an evaluation of biodistribution in mice bearing S180 tumors indicated that all of the complexes could accumulate in the tumors. Among them, Tc-99m-2c exhibited the highest tumor uptake and tumor/blood and tumor/muscle ratios at 2 h post-injection. Further, single photon emission computed tomography (SPECT) imaging studies indicated clear accumulation in tumors, suggesting that Tc-99m-2c was a promising candidate for hypoxia imaging.

• 出版日期2018-6-1
• 单位北京师范大学