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Synthesis, Tc-radiolabeling and in vivo evaluation of a new sulphonamide derivative for solid tumor imaging

Journal of Radioanalytical and Nuclear Chemistry, ISSN: 1588-2780, Vol: 326, Issue: 1, Page: 129-136
2020
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Article Description

A novel sulphonamide derivative (EPBS) was prepared at high yield and characterized by H NMR and infrared radiation spectroscopy. Its cytotoxic activity was examined in breast carcinoma (MCF-7) cells at a dose of 25 μg/mL. Approximately 68 percent effective inhibition has been achieved. Furthermore, the synthesized ligand was directly radiolabeled with technetium-99m using sodium borohydride. High radiochemical purities (95.5%) were determined using radio-paper chromatography and electrophoresis. Its in vivo evaluation in tumor bearing mice demonstrated a high tumor uptake of the Tc-EPBS complex at 30 min post injection (6.74%) and tumor/muscle (T/NT) ratio equal to 5.04 ± 0.05. In conclusion, Tc-EPBS agent showed favorable characteristics for the radio-diagnosis of solid tumors.

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