Thiadiazole derivatives have garnered significant attention in the field of medicinal chemistry due to their diverse pharmacological activities, including anticancer properties. This article presents the synthesis of a series of thiadiazole derivatives and investigates their chemical characterization and potential anticancer effects on various cell lines. The results of the nuclear magnetic resonance (NMR) analyses confirmed the successful formation of the target compounds. The anticancer potential was evaluated through in silico and in vitro cell-based assays using LoVo and MCF-7 cancer lines. The assays included cell viability, proliferation, apoptosis, and cell cycle analysis to assess the compounds’ effects on cancer cell growth and survival. Daphnia magna was used as an invertebrate model for the toxicity evaluation of the compounds. The results revealed promising anticancer activity for several of the synthesized derivatives, suggesting their potential as lead compounds for further drug development. The novel compound 2g, 5-[2-(benzenesulfonylmethyl)phenyl]-1,3,4-thiadiazol-2-amine, demonstrated good anti-proliferative effects, exhibiting an IC50 value of 2.44 µM against LoVo and 23.29 µM against MCF-7 after a 48-h incubation and little toxic effects in the Daphnia test.

中文翻译：

---

1,3,4-噻二唑衍生物的合成及其抗癌评价


噻二唑衍生物因其多种药理活性（包括抗癌特性）而在药物化学领域引起了广泛关注。本文介绍了一系列噻二唑衍生物的合成，并研究了它们的化学特性和对各种细胞系的潜在抗癌作用。核磁共振（NMR）分析结果证实目标化合物的成功形成。使用 LoVo 和 MCF-7 癌细胞系通过计算机和体外细胞测定评估了抗癌潜力。这些测定包括细胞活力、增殖、凋亡和细胞周期分析，以评估化合物对癌细胞生长和存活的影响。使用大型溞作为无脊椎动物模型来评估化合物的毒性。结果显示，几种合成衍生物具有良好的抗癌活性，表明它们作为进一步药物开发的先导化合物的潜力。新型化合物2g, 5-[2-(苯磺酰甲基)苯基]-1,3,4-噻二唑-2-胺表现出良好的抗增殖作用，对LoVo的IC50值为2.44 µM，对MCF-的IC50值为23.29 µM。 7 孵化48小时后，在水蚤测试中几乎没有毒性作用。