新型[99mTc（I）] +和[99mTc（I）（CO）3] +配合物与4-硝基咪唑异氰酸酯的放射性合成和评估，可用于影像学低氧,Applied Organometallic Chemistry

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新型[99mTc（I）] +和[99mTc（I）（CO）3] +配合物与4-硝基咪唑异氰酸酯的放射性合成和评估，可用于影像学低氧
Applied Organometallic Chemistry ( IF 3.7 ) Pub Date : 2020-05-15 , DOI: 10.1002/aoc.5798
Qing Ruan ₁ , Xuran Zhang ₁ , Junbo Zhang ₁

Affiliation

具有异氰酸酯的[ ^99m Tc（I）] ⁺和[ ^99m Tc（I）（CO）₃ ] ⁺配合物具有很高的稳定性，这使其成为开发新型^99m Tc放射性药物的合适平台。为了开发用于成像低氧的新型^99m Tc放射性示踪剂，在这项研究中，合成了一种新型L配体（4-硝基咪唑异氰酸酯衍生物），并使用[ ^99m Tc（I）] ⁺核心和[ ^99m Tc（I）（CO）₃标记] ⁺核心产生[ ^99m Tc（L）₆ ] ⁺和[ ^99mTc（CO）₃（L）₃ ] ⁺具有高产率。为了验证^99m Tc配合物的结构，合成并表征了相应的rh类似物。两种^99m Tc络合物均稳定且亲水。体外细胞摄取结果表明它们可以表现出良好的低氧选择性。对患有S180肿瘤的小鼠的生物分布的评估表明，它们都可以在肿瘤中蓄积。它们之间的[ ^99m Tc（L）₆ ] ⁺表现出比[ ^99m Tc（CO）₃（L）₃ ] ⁺更高的肿瘤吸收和肿瘤/非靶标比率。此外，[ ^99m Tc（L）₆ ] ^+的单光子发射计算机断层扫描（SPECT）成像研究表明，肿瘤中明显积聚，并且肿瘤部位吸收的感兴趣区（ROI）比值对相应的非肿瘤区域为5.64±0.52。以上结果表明[ ^99m Tc（L）₆ ] ⁺将成为成像肿瘤缺氧的潜在示踪剂。

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Radiosynthesis and evaluation of novel [99mTc(I)]+ and [99mTc(I)(CO)3]+ complexes with a 4‐nitroimidazole isocyanide for imaging tumor hypoxia

[^99mTc(I)]⁺ and [^99mTc(I)(CO)₃]⁺ complexes with isocyanide exhibit high stability, which makes them suitable platforms to develop novel ^99mTc radiopharmaceuticals. To develop novel ^99mTc radiotracers for imaging hypoxia, in this study, a novel L ligand (4‐nitroimidazole isocyanide derivative) was synthesized and labelled using [^99mTc(I)]⁺ core and [^99mTc(I)(CO)₃]⁺ core to produce [^99mTc(L)₆]⁺ and [^99mTc(CO)₃(L)₃]⁺ with high yields. To verify the structure of the ^99mTc complexes, corresponding rhenium analogues were synthesized and characterized. Both of the ^99mTc complexes were stable and hydrophilic. in vitro cellular uptake results showed they could exhibit good hypoxic selectivity. The evaluation of biodistribution in mice bearing S180 tumors indicated both of them could accumulate in tumor. Between them, [^99mTc(L)₆]⁺ exhibited higher tumor uptake and tumor/non‐target ratio than [^99mTc(CO)₃(L)₃]⁺. Further, single photon emission computed tomography (SPECT) imaging studies of [^99mTc(L)₆]⁺ indicated an obvious accumulation in tumor and the value of the region‐of‐interest (ROI) ratio of the uptake for the tumor site to the corresponding non‐tumor region was 5.64 ± 0.52. The above results suggested [^99mTc(L)₆]⁺ would be a potential tracer for imaging tumor hypoxia.

更新日期：2020-05-15

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