Preparation of two 99mTc(CO)3 labelled complexes with a 4-nitroimidazole isocyanide at different temperatures for molecular imaging of tumor hypoxia
Preparation of two 99mTc(CO)3 labelled complexes with a 4-nitroimidazole isocyanide at different temperatures for molecular imaging of tumor hypoxia
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DOI：
10.1007/s10967-019-07005-7
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发表时间：
2020-01
影响因子：
1.6
通讯作者：
Q. Ruan;Xuran Zhang;Qianqian Gan;Si’an Fang;Junbo Zhang
中科院分区：
文献类型：
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作者：
Q. Ruan;Xuran Zhang;Qianqian Gan;Si’an Fang;Junbo Zhang
合成了一种4-硝基咪唑异腈衍生物（6），并以99 mTc（CO）3为核进行了标记。99 mTc（CO）3-6a和99 mTc（CO）3- 6 b分别在100 °C和25 °C下制备，99 mTc（CO）3-6a含有3个6分子，而99 mTc（CO）3- 6 b含有2个6分子。制备了相应的99 mTc配合物，证实了99 mTc配合物的结构。两种配合物均表现出良好的体外稳定性和低氧选择性。分配系数结果表明，两者均为亲水性，且99 mTc（CO）3-6a比99 mTc（CO）3- 6 b更亲水。根据生物分布研究结果，99 mTc（CO）3-6a在注射后2小时显示出较高的肿瘤/血液和肿瘤/肌肉比率。此外，单光子发射计算机断层扫描（SPECT）研究99 mTc（CO）3-6a显示了可观察到的肿瘤摄取，这表明它可能是一种潜在的肿瘤乏氧显像示踪剂。
A 4-nitroimidazole isocyanide derivative (6) was synthesized and radiolabelled with99mTc(CO)3core in high yield. It was interesting to note that99mTc(CO)3-6a and99mTc(CO)3-6b can be prepared at 100 °C and 25 °C, respectively.99mTc(CO)3-6a had three6molecules while99mTc(CO)3-6b contained two6molecules. The corresponding rhenium complexes were prepared to confirm the structure of the99mTc complexes. Both complexes showed good stability in vitro and hypoxic selectivity. The partition coefficient results indicated both of them were hydrophilic and99mTc(CO)3-6a was more hydrophilic than99mTc(CO)3-6b. From the biodistribution study results,99mTc(CO)3-6a showed higher tumor/blood and tumor/muscle ratios at 2 h post-injection. Further, single photon emission computed tomography (SPECT) imaging study of99mTc(CO)3-6a showed there was an observable tumor uptake, suggesting it would be a potential tracer for imaging of tumor hypoxia.