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

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.