Novel 99mTc labelled complexes with 2-nitroimidazole isocyanide: design, synthesis and evaluation as potential tumor hypoxia imaging agents,RSC Medicinal Chemistry

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Novel 99mTc labelled complexes with 2-nitroimidazole isocyanide: design, synthesis and evaluation as potential tumor hypoxia imaging agents
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-05-07 00:00:00 , DOI: 10.1039/c8md00146d
Qing Ruan ₁ , Xuran Zhang ₁ , Xiao Lin _{1,

2} , Xiaojiang Duan ₁ , Junbo Zhang ₁

Affiliation

Radiolabelled 2-nitroimidazoles have been used for imaging hypoxia. With the aim of developing novel ^99mTc 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 ^99mTc complexes. These ^99mTc 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, ^99mTc-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 ^99mTc-2c was a promising candidate for hypoxia imaging.

中文翻译：

新型 99mTc 标记的 2-硝基咪唑异氰化物复合物：作为潜在肿瘤缺氧显像剂的设计、合成和评估

放射性标记的 2-硝基咪唑已用于缺氧成像。为了开发用于缺氧成像的新型^99m Tc放射性示踪剂，合成了四种新型2-硝基咪唑异氰化物衍生物（2a、2b、2c和2d ），并进行放射性标记以制备其相应的^99m Tc配合物。这些^99m Tc 配合物在体外稳定，并且具有良好的缺氧选择性。分配系数结果表明它们是亲水性的，并且对携带S180肿瘤的小鼠的生物分布评估表明所有复合物都可以在肿瘤中积聚。其中，^99m Tc- 2c在注射后2小时表现出最高的肿瘤摄取以及肿瘤/血液和肿瘤/肌肉比率。此外，单光子发射计算机断层扫描 (SPECT) 成像研究表明肿瘤中存在明显的积累，表明^99m Tc- 2c是缺氧成像的有希望的候选者。

更新日期：2018-05-07

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