This work presents the synthesis and characterization of eight copper complexes [Cu(L-dipeptide)(neo)]·nH2O (neo = neocuproine) and their cytotoxic activities against tumor cell lines. The crystalline structure of [Cu(gly-val)(neo)]·3H2O, [Cu(gly-leu)(neo)]·H2O, [Cu(ala-gly)(neo)]·4H2O, [Cu(val-phe)(neo)]·4.5H2O and [Cu(phe-phe)(neo)]·3H2O were determined by single crystal X-ray diffraction. In all of them, the Cu(II) is pentacoordinated, in a square pyramidal environment. The coordination observed in solid state was retained in the major species in aqueous solution, as suggested by Electronic Paramagnet Resonance and UV-vis spectroscopies. The complexes were shown to have affinity for isolated DNA, as determined by Circular Dichroism experiments. Furthermore, biological experiments showed that all the complexes present high cytotoxic activity against the cell lines: MDA-MB-231, MCF-7 (human metastatic breast adenocarcinomas, the first triple negative), MCF-10A (human normal breast cells), A549 (human lung epithelial carcinoma) and MRC-5 (human lung epithelial cells). Together, these results suggest that these compounds are promising steps towards new effective drugs to treat cancer.

中文翻译：

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一系列三元铜（II）-L-二肽-新古铜配合物的合成和结构表征。研究它们对包括MDA-MB-231三重阴性乳腺癌细胞在内的癌细胞的细胞毒性。

这项工作介绍了八种铜配合物[Cu（L-二肽）（neo）]·nH2O（neo = neocuproine）的合成和表征，以及它们对肿瘤细胞系的细胞毒活性。[Cu（gly-val）（neo）]·3H2O，[Cu（gly-leu）（neo）]·H2O，[Cu（ala-gly）（neo）]·4H2O，[Cu（val通过单晶X射线衍射测定-（phe）（neo）]·4.5H 2 O和[Cu（phe-phe）（neo）]·3H 2O。在所有这些中，Cu（II）在方形锥体环境中是五配位的。固态观察到的配位保留在水溶液中的主要物质中，如电子顺磁共振和紫外可见光谱所表明的。通过圆二色性实验确定，该复合物对分离的DNA具有亲和力。此外，生物学实验表明，所有复合物均具有针对细胞系的高细胞毒活性：MDA-MB-231，MCF-7（人类转移性乳腺癌），首批三阴性，MCF-10A（人类正常乳腺细胞），A549（人类）肺上皮癌）和MRC-5（人肺上皮细胞）。总之，这些结果表明这些化合物是朝着治疗癌症的新有效药物迈出的有前途的步骤。