该研究旨在合成一种基于铂（thioPt）的新型双（缩氨基硫脲）衍生物，并评估其对 MFC-7 和 MDA-MB-231 乳腺癌细胞的抗癌特性。在 K2CO3 存在下，K2PtCl4 与 2,2'-(1,2-二苯基乙烷-1,2-二亚基)双(肼-1-硫代甲酰胺)在乙醇中反应合成了一种新的铂配合物。在获得的配合物中，铂原子通过共轭体系配位=N-NC-S-。使用NMR光谱、HR MS、IR和X射线结构分析对新化合物的结构进行了表征。细胞毒性测定结果表明，化合物thioPt具有有效的抗癌活性（MCF-7：61.03 ± 3.57 µM，MDA-MB-231：60.05 ± 5.40 µM），即使与正常MCF-10A乳腺上皮细胞相比，其毒性也较小。对照化合物（顺铂）。此外，后续实验发现thioPt通过外在（↑caspase 8活性）和内在（↓ΔΨm）途径诱导细胞凋亡，最终导致活性caspase 3/7水平增加。在暴露于一定浓度的测试化合物（thio、thioPt、cisPt）的 MCF-7 和 MDA-MB-231 乳腺癌细胞中，检查了自噬的诱导以及参与该过程的蛋白质（LC3A/B 和 Beclin-1）水平50 µM，持续 24 小时。基于这些结果，可以得出结论，thio 和 thioPt 不会显着影响自噬过程。这证明了它们相对于顺铂的优越性，顺铂可以通过刺激自噬来刺激癌细胞存活。版权所有 © 2024 作者。由爱思唯尔公司出版。保留所有权利。

The study aims to synthesize a novel bis(thiosemicarbazone) derivative based on platinum (thioPt) and evaluate its anticancer properties against MFC-7 and MDA-MB-231 breast cancer cells. A new platinum complex was synthesised by reacting K2PtCl4 with 2,2'-(1,2-diphenylethane-1,2-diylidene)bis(hydrazine-1-carbothioamide) in ethanol in the presence of K2CO3. In the obtained complex, the platinum atom is coordinated by a conjugated system = N-NC-S-The structures of the new compound were characterised using NMR spectroscopy, HR MS, IR, and X-ray structural analysis. The obtained results of the cytotoxicity assay indicate that compound thioPt had potent anticancer activity (MCF-7: 61.03 ± 3.57 µM, MDA-MB-231: 60.05 ± 5.40 µM) with less toxicity against normal MCF-10A breast epithelial cells, even compared to the reference compound (cisplatin). In addition, subsequent experiments found that thioPt induces apoptosis through both an extrinsic (↑caspase 8 activity) and intrinsic (↓ΔΨm) pathway, which ultimately leads to an increase in active caspase 3/7 levels. The induction of autophagy and levels of proteins involved in this process (LC3A/B and Beclin-1) were examined in MCF-7 and MDA-MB-231 breast cancer cells exposed to tested compounds (thio, thioPt, cisPt) at a concentration of 50 µM for 24 h. Based on these results, it can be concluded that thio and thioPt do not significantly affect the autophagy process. This demonstrates their superiority over cisplatin, which can stimulate cancer cell survival through its effect on stimulation of autophagy.Copyright © 2024 The Author(s). Published by Elsevier Inc. All rights reserved.