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.