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Synthesis and cellular uptake of p ‐[ 123 I]‐phenyl‐amino‐thiazole ( 123 I‐PAT) as a potential agent for targeting tubulin polymerization in tumors
Author(s) -
Wang DaMing,
Kuo JiaWei,
Kuo WeiTi,
Hsu ChengFang,
Wang MeiHui,
Chang Yu,
Lin WuuJyh,
Wang JenTsung
Publication year - 2014
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3178
Subject(s) - chemistry , thiazole , polymerization , electrophile , iodide , tubulin , stereochemistry , radiochemistry , microtubule , combinatorial chemistry , biochemistry , organic chemistry , catalysis , polymer , biology , microbiology and biotechnology
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.