Smoleński Piotr, Śliwińska-Hill Urszula, Kwiecień Anna, Wolińska Joanna, Poradowski Dominik
Faculty of Chemistry, University of Wrocław, F. Joliot-Curie 14, 50-383 Wrocław, Poland.
Department of Basic Chemical Sciences, Faculty of Pharmacy, Wrocław Medical University, Borowska 211a, 50-556 Wrocław, Poland.
Molecules. 2024 Feb 21;29(5):945. doi: 10.3390/molecules29050945.
This study presents a simple and energy-efficient self-assembly LAG synthetic method for novel water-soluble copper(I) complexes [Cu(terpy)(PTA)][PF] () and [Cu(terpy)(PTA)][PF] (). They were characterized by FT-IR, H, and P{H} NMR spectroscopy, elemental analysis, and single-crystal/powder X-ray diffraction (for ). The X-ray analysis of compound indicates a bidentate coordination mode of terpyridine to the metal center. Variable-temperature NMR tests indicate dynamic properties for terpyridine in the case of both compounds, as well as for the PTA ligands in the case of . Additionally, compounds and exhibit interesting cytotoxic activity, which was tested on normal human dermal fibroblasts (NHDFs), human lung carcinoma (A549), human breast adenocarcinoma (MCF-7), and human cervix carcinoma (HeLa) established cell lines. In comparison to the other tested compounds, complexes and seem to have significantly lower IC values against cancer cells (A549, HeLa, MCF-7), indicating their potential as prospective anticancer agents. Moreover, both compounds show no significant toxicity towards normal skin cells (NHDFs), suggesting a certain selectivity in their action on cancer cells. Cisplatin as a reference compound also exhibited considerable cytotoxicity against cancer cells but with a low level of selectivity, which could lead to unwanted effects on normal cells. Remarkably, compounds and exhibit up to 30 times the cytotoxic activity of cisplatin, with a six-fold lower toxicity to normal cells. They also interact strongly with human serum albumin, suggesting potential therapeutic applications. Overall, these compounds hold significant promise as potential chemotherapeutic agents.
本研究提出了一种简单且节能的自组装LAG合成方法，用于制备新型水溶性铜（I）配合物[Cu（terpy）（PTA）][PF]（）和[Cu（terpy）（PTA）][PF]（）。通过傅里叶变换红外光谱（FT-IR）、氢谱（H）和磷谱{H}核磁共振光谱（P{H} NMR）、元素分析以及单晶/粉末X射线衍射（针对）对它们进行了表征。化合物的X射线分析表明，三联吡啶与金属中心呈双齿配位模式。变温核磁共振测试表明，在这两种化合物中三联吡啶都具有动态特性，在中PTA配体也具有动态特性。此外，化合物和表现出有趣的细胞毒性活性，该活性在正常人皮肤成纤维细胞（NHDFs）、人肺癌（A549）、人乳腺腺癌（MCF-7）和人宫颈癌（HeLa）等已建立的细胞系上进行了测试。与其他测试化合物相比，配合物和对癌细胞（A549、HeLa、MCF-7）的半数抑制浓度（IC）值似乎显著更低，表明它们作为潜在抗癌剂的潜力。此外，这两种化合物对正常皮肤细胞（NHDFs）均无明显毒性，表明它们对癌细胞的作用具有一定的选择性。作为参考化合物的顺铂对癌细胞也表现出相当大的细胞毒性，但选择性较低，这可能会对正常细胞产生不良影响。值得注意的是，化合物和的细胞毒性活性高达顺铂的30倍，对正常细胞的毒性低六倍。它们还与人血清白蛋白强烈相互作用，表明具有潜在的治疗应用。总体而言，这些化合物作为潜在的化疗药物具有重大前景。
