RESUMEN
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.
Asunto(s)
Compuestos de Anilina/síntesis química , Compuestos de Anilina/farmacología , Multimerización de Proteína/efectos de los fármacos , Tiazoles/síntesis química , Tiazoles/farmacología , Moduladores de Tubulina/síntesis química , Moduladores de Tubulina/farmacología , Tubulina (Proteína)/química , Compuestos de Anilina/metabolismo , Transporte Biológico , Línea Celular Tumoral , Técnicas de Química Sintética , Humanos , Estructura Cuaternaria de Proteína , Tiazoles/metabolismo , Moduladores de Tubulina/metabolismoRESUMEN
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.