Abstract
This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of [99mTc(CO)3(IDA–PEG3–CB)]−. The novel chlorambucil derivative was successfully synthesized by conjugation of iminodiacetic acid (IDA) to chlorambucil via a pegylated linker. The ligand could be labeled by [99mTc(CO)3]+ core in high yield to get [99mTc(CO)3(IDA–PEG3–CB)]−, which was very hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [99mTc(CO)3(IDA–PEG3–CB)]− accumulated in the tumor with favorable uptake and retention. The good accumulation in tumor tissue with high tumor/muscle ratios warrants further research to improve tumor targeting efficacy and pharmacokinetic profile of radiolabeled chlorambucil derivative by structural modification.
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Acknowledgments
The work was financially supported by the Fundamental Research Funds for the Central Universities (lzujbky-2009-22), Chunhui Plan (Z2008-1-62018) Sponsored by Ministry of Education, China and Ph.D. Programs Foundation of Ministry of Education of China (20090211120026).
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Wang, J., Yang, J., Yan, Z. et al. Synthesis and preliminary biological evaluation of [99mTc(CO)3(IDA–PEG3–CB)]− for tumor imaging. J Radioanal Nucl Chem 287, 465–469 (2011). https://doi.org/10.1007/s10967-010-0702-6
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DOI: https://doi.org/10.1007/s10967-010-0702-6