title: Synthesis and cellular uptake of p-[(123)I]-phenyl-amino-thiazole ((123)I-PAT) as a potential agent for targeting tubulin polymerization in tumors.
abstract: 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.
authors.affiliation: Chemistry Division, Institute of Nuclear Energy Research, Longtan, Taoyuan, 325, Taiwan.
authors.forename: Da-Ming
authors.initials: DM
authors.lastname: Wang
authors.forename: Jia-Wei
authors.initials: JW
authors.lastname: Kuo
authors.forename: Wei-Ti
authors.initials: WT
authors.lastname: Kuo
authors.forename: Cheng-Fang
authors.initials: CF
authors.lastname: Hsu
authors.forename: Mei-Hui
authors.initials: MH
authors.lastname: Wang
authors.forename: Yu
authors.initials: Y
authors.lastname: Chang
authors.forename: Wuu-Jyh
authors.initials: WJ
authors.lastname: Lin
authors.forename: Jen-Tsung
authors.initials: JT
authors.lastname: Wang
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D001692:Biological Transport; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D006801:Humans; D055503:Protein Multimerization / Q000187:drug effects*; D020836:Protein Structure, Quaternary; D013844:Thiazoles / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D014404:Tubulin / Q000737:chemistry*; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*
chemical_list: C000593186:2-(4-iodophenylamino)thiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone; D000814:Aniline Compounds; D013844:Thiazoles; D014404:Tubulin; D050257:Tubulin Modulators
keywords: iodine-123; phenyl-amino-thiazoles; radioiodinated analog; tubulin polymerization