A novel sulphonamide derivative (EPBS) was prepared at high yield and characterized by 1H 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 99mTc-EPBS complex at 30 min post injection (6.74%) and tumor/muscle (T/NT) ratio equal to 5.04 ± 0.05. In conclusion, 99mTc-EPBS agent showed favorable characteristics for the radio-diagnosis of solid tumors.

中文翻译：

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用于实体瘤成像的新型磺胺衍生物的合成、99mTc 放射性标记和体内评价

以高产率制备了一种新型磺酰胺衍生物 (EPBS)，并通过 1 H NMR 和红外辐射光谱对其进行了表征。在乳腺癌 (MCF-7) 细胞中以 25 μg/mL 的剂量检查其细胞毒活性。已经实现了大约 68% 的有效抑制。此外，合成的配体使用硼氢化钠直接用锝 99m 进行放射性标记。使用放射纸色谱法和电泳法测定了高放射化学纯度 (95.5%)。其在荷瘤小鼠中的体内评估表明，在注射后 30 分钟 (6.74%) 和肿瘤/肌肉 (T/NT) 比率等于 5.04 ± 0.05 时，99mTc-EPBS 复合物的肿瘤吸收率很高。总而言之，99mTc-EPBS 试剂显示出对实体瘤的放射诊断有利的特性。