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  • Author or Editor: Tingting Niu x
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Abstract  

This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of the 99mTc(CO)3–AOPA colchicine conjugate. The novel ligand was successfully synthesized by conjugation of N-(acetyloxy)-2-picolylamino (AOPA) to deacetylcolchicine via a short carbonyl-methylene linker. Radiolabeling was performed in high yield with [99mTc(CO)3]+ core. 99mTc(CO)3–AOPA colchicine conjugate was hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that 99mTc(CO)3–AOPA colchicine conjugate accumulated in the tumor with good uptake and retention. However, its clearance from normal organs was not so fast, resulting in poor T/NT ratios. Further modification on the linker or/and 99mTc-chelate to improve the tumor targeting efficacy and in vivo kinetic profiles is currently in progress.

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Abstract  

This work reports the synthesis and preliminary biodistribution results of [131I]SIB-PEG4-CHC in tumor-bearing mice. The tributylstannyl precursor ATE-PEG4-CHC was synthesized by conjugation of ATE to amino pegylated colchicine NH2-PEG4-CHC. [131I]SIB-PEG4-CHC was radiosynthesized by electrophilic destannylation of the precursor with a yield of ~44%. The radiochemical purity (RCP) appeared to be >95% by a Sep-Pak cartridge purification. [131I]SIB-PEG4-CHC was lipophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [131I]SIB-PEG4-CHC cleared from background rapidly, and didn’t deiodinate in vivo. However, the poor tumor localization excluded it from further investigations as a tumor-targeted radiopharmaceuticals.

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