Thidiazuron (TDZ) was reported to possess anti-cancer activity against Human cervical carcinoma cell line, so that this study has been conducted for the radiolabeling of TDZ with Technetium-99m. The conditions of the radiolabeling process were optimized and a high radiochemical yield of 93.1 ± 0.35% has been obtained. Molecular docking study illustrated that [99mTc]technetium bisthiadiazuron (99mTc-TDZ) complex has the ability to bind with Caspase-3 protein that over expressed in cancers. Its in-vivo biodistribution on solid tumor bearing mice showed comparatively high T/NT ratio of 6.87 ± 0.14 at 60 min post injection. These promising characteristics make our new designed labeled conjugate a very suitable candidate for molecular imaging of solid tumors, particularly in the cervix.

中文翻译：

---

99mTc-Thiadiazuron作为宫颈癌成像新潜在药物的分子对接和初步生物评价

据报道，噻二唑隆 (TDZ) 对人宫颈癌细胞系具有抗癌活性，因此本研究已针对使用锝 99m 对 TDZ 进行放射性标记。优化了放射性标记过程的条件，获得了 93.1 ± 0.35% 的高放射化学产率。分子对接研究表明，[99mTc]锝双硫脲 (99mTc-TDZ) 复合物具有与癌症中过度表达的 Caspase-3 蛋白结合的能力。在注射后 60 分钟，它在携带实体瘤的小鼠体内的体内生物分布显示出相对较高的 T/NT 比为 6.87 ± 0.14。这些有前途的特性使我们新设计的标记缀合物非常适合实体肿瘤的分子成像，尤其是在子宫颈中。