Preparation of two 99mTc(CO)3 labelled complexes with a 4-nitroimidazole isocyanide at different temperatures for molecular imaging of tumor hypoxia

A 4-nitroimidazole isocyanide derivative ( 6 ) was synthesized and radiolabelled with 99m Tc(CO) 3 core in high yield. It was interesting to note that 99m Tc(CO) 3 -6a and 99m Tc(CO) 3 -6b can be prepared at 100 °C and 25 °C, respectively. 99m Tc(CO) 3 -6a had three 6 molecules while 99m Tc(CO) 3 -6...

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Bibliographic Details
Published in:Journal of radioanalytical and nuclear chemistry 2020, Vol.323 (2), p.851-859
Main Authors: Ruan, Qing, Zhang, Xuran, Gan, Qianqian, Fang, Si’an, Zhang, Junbo
Format: Article
Language:English
Subjects:
Chemistry
Chemistry and Materials Science
Computed tomography
Diagnostic Radiology
Emission analysis
Hadrons
Heavy Ions
Hydrophilicity
Hypoxia
Imaging
Inorganic Chemistry
Muscles
Nuclear Chemistry
Nuclear Physics
Photon emission
Physical Chemistry
Rhenium
Selectivity
Tomography
Tumors
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Summary:A 4-nitroimidazole isocyanide derivative ( 6 ) was synthesized and radiolabelled with 99m Tc(CO) 3 core in high yield. It was interesting to note that 99m Tc(CO) 3 -6a and 99m Tc(CO) 3 -6b can be prepared at 100 °C and 25 °C, respectively. 99m Tc(CO) 3 -6a had three 6 molecules while 99m Tc(CO) 3 -6b contained two 6 molecules. The corresponding rhenium complexes were prepared to confirm the structure of the 99m Tc complexes. Both complexes showed good stability in vitro and hypoxic selectivity. The partition coefficient results indicated both of them were hydrophilic and 99m Tc(CO) 3 -6a was more hydrophilic than 99m Tc(CO) 3 -6b. From the biodistribution study results, 99m Tc(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 of 99m Tc(CO) 3 -6a showed there was an observable tumor uptake, suggesting it would be a potential tracer for imaging of tumor hypoxia.
ISSN:0236-5731
1588-2780
DOI:10.1007/s10967-019-07005-7