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Synthesis and bioevaluation of novel radioiodinated PEG-modified 2-nitroimidazole derivatives for tumor hypoxia imaging

  • Fan Wang
  • Xianteng Yang
  • Hua Zhu
  • Zhi Yang
  • Taiwei ChuEmail author
Article
  • 4 Downloads

Abstract

Two novel radioiodinated PEG-modified 2-nitromidazole derivatives were prepared. The two radiotracers demonstrate good stability in vitro. In the cellular uptake experiments, the uptakes in hypoxic condition are higher than those in aerobic condition for two radiotracers. The biodistribution results in mice bearing S180 tumor demonstrate the uptakes of the two radiotracers in tumor show maximum at 1 h. The two radiotracers could be eliminated quickly from normal tissue. In SPECT/CT imaging study, the tumor could be observed clearly in S180 tumor using the two radiotracers. These results suggest they are worth of further study as potential hypoxia imaging agents.

Keywords

2-Nitroimidazole 2-(4′-Aminophenyl)benzothiazole Tumor Hypoxia imaging 

Notes

Acknowledgements

This work was supported by the National Natural Science Foundation of China (Grant Nos. 11575010 and 21371017).

Supplementary material

10967_2019_6649_MOESM1_ESM.docx (5.9 mb)
Supplementary material 1 (DOCX 5991 kb)

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Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2019

Authors and Affiliations

  1. 1.Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, College of Chemistry and Molecular EngineeringPeking UniversityBeijingChina
  2. 2.Medical CollegeGuizhou UniversityGuiyangChina
  3. 3.Department of OrthopaedicsGuizhou Provincial People’s HospitalGuiyangChina
  4. 4.Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear MedicinePeking University Cancer Hospital and InstituteBeijingChina

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