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.
Subject(s)
Aniline Compounds/chemical synthesis , Aniline Compounds/pharmacology , Protein Multimerization/drug effects , Thiazoles/chemical synthesis , Thiazoles/pharmacology , Tubulin Modulators/chemical synthesis , Tubulin Modulators/pharmacology , Tubulin/chemistry , Aniline Compounds/metabolism , Biological Transport , Cell Line, Tumor , Chemistry Techniques, Synthetic , Humans , Protein Structure, Quaternary , Thiazoles/metabolism , Tubulin Modulators/metabolismABSTRACT
The preparation of a novel fluorescent lipid II-based substrate for transglycosylases (TGases) is described. This substrate has characteristic structural features including a shorter lipid chain, a fluorophore tag at the end of the lipid chain rather than on the peptide chain, and no labeling with a radioactive atom. This fluorescent substrate is readily utilized in TGase activity assays to characterize TGases and also to evaluate the activities of TGase inhibitors.
