Synthesis and cellular uptake of p-[(123)I]-phenyl-amino-thiazole ((123)I-PAT) as a potential agent for targeting tubulin polymerization in tumors

The phenyl-amino-thiazole (PAT) templates of methoxylbenzoyl-aryl-thiazole are potent agents against cancer by inhibiting tubulin polymerization in the nanomolar range. Herein, a radioiodinated PAT, [(123)I]-PAT 1, was prepared via a tributylstannyl precursor and [(123)I]iodide through electrophilic aromatic radioiodination. Radiolabelling of [(123)I]-PAT 1 was achieved in less than 15 min, with a radiochemical purity of over 99%. The accumulated radioactivity in tumor cellular uptake experiments suggested that [(123) I]-PAT could serve as a potential radioprobe for targeting tumor cells.