经典无机配位化合物顺铂（cis-[Pt(NH3)2Cl2]）作为第一种抗癌金属药物的成功开启了致力于发现具有抗肿瘤活性的配位化合物（涵盖各种金属）的研究领域。其中，铜配合物已成为开发治疗癌症药物的有趣候选者。在这项工作中，合成了 Cu(II) 与二亚胺（菲咯啉或 4-甲基菲咯啉）和 3-(4-羟苯基)丙酸酯、苯基羧酸酯或苯基乙酸酯的混合配体配合物。它们在固态下进行了表征，包括[Cu2(3-(4-羟基苯基)丙酸酯)3(菲咯啉)2]Cl·H2O的新晶体结构。获得的配合物呈现出多种化学计量。在溶液中，配合物部分解离成相应的铜-二亚胺配合物。通过圆二色性、相对粘度变化和紫外-可见滴定评估，复合物通过部分嵌入和凹槽结合与 DNA 结合。体外测定了复合物对 MDA-MB-231、MCF-7（人转移性乳腺腺癌，第一个三阴性）、MCF-10A（乳腺非肿瘤）、A549（人肺上皮癌）和 MRC- 的细胞毒性。 5（人非肿瘤肺上皮细胞），发现其活性高于顺铂，但选择性较低。版权所有 © 2024 Elsevier Inc. 保留所有权利。

The success of a classic inorganic coordination compound, Cisplatin, cis-[Pt(NH3)2Cl2], as the first anticancer metallodrug started a field of research dedicated to discovering coordination compounds with antitumor activity, encompassing various metals. Among these, copper complexes have emerged as interesting candidates to develop drugs to treat cancer. In this work, mixed ligand complexes of Cu(II) with diimines (phenanthroline or 4-methylphenanthroline) and 3-(4-hydroxyphenyl)propanoate, phenylcarboxylate or phenylacetate were synthesized. They were characterized in the solid state, including a new crystal structure of [Cu2(3-(4-hydroxyphenyl)propanoate)3(phenanthroline)2]Cl·H2O. The obtained complexes presented a variety of stoichiometries. In solution, complexes were partially dissociated in the corresponding Cu-diimine complex. The complexes bound to the DNA by partial intercalation and groove binding, as assessed by Circular Dichroism, relative viscosity change and UV-Vis titration. The cytotoxicity of the complexes was determined in vitro on MDA-MB-231, MCF-7 (human metastatic breast adenocarcinomas, the first triple negative), MCF-10A (breast nontumoral), A549 (human lung epithelial carcinoma), and MRC-5 (human nontumoral lung epithelial cells), finding an activity higher than that of Cisplatin, although with less selectivity.Copyright © 2024 Elsevier Inc. All rights reserved.