研究动态
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含呋喃芳酰腙配体的铜 (II) 配合物:合成、结构研究、溶液化学以及与 HSA 的相互作用。

Copper(II) complexes of a furan-containing aroylhydrazonic ligand: syntheses, structural studies, solution chemistry and interaction with HSA.

发表日期:2023 Nov 02
作者: Fagner da Silva Moura, Ygor S Sobrinho, Carolina Stellet, Jilder D P Serna, Carolina B P Ligiero, Maurício I Yoguim, Daphne S Cukierman, Renata Diniz, Odivaldo C Alves, Nelson H Morgon, Aguinaldo R de Souza, Nicolás A Rey
来源: PHYSICAL THERAPY & REHABILITATION JOURNAL

摘要:

由于其多靶点作用模式,铜(II)配合物已成为癌症治疗中铂类药物的潜在替代品。在此背景下,我们报道了该元素 1 和 2 的新型单核和双核配位化合物的合成,这些化合物衍生自配体 5-甲基水杨醛 2-呋喃酰腙 (H2L)。所有三种化合物均在固态和溶液中进行了结构和光谱表征。在1中,Cu由来自腙配体的三个供体原子和一个氯离子配位。 H2L 在酚氧处被去质子化。另一方面,双核配合物 2 是 1 的二聚形式,其中一对单核单元的氯离子丢失,苯氧桥取代其位置,双连接金属中心并产生具有配体完全去质子化。该化合物在室温下在水性介质中相当稳定。实验-理论相结合的方法表明,它们都能够结合人血清白蛋白(HSA),尽管在不同的位点并且具有不同的化学计量和亲和力(根据计算的结合能得出结论)。鉴于此,并且由于含腙铜配合物众所周知的抗增殖活性,我们认为这里提出的化合物很有前途,并相信它们值得进行更深入的研究,以评估其对抗肿瘤细胞系的潜力。
Copper(II) complexes have become a potential alternative to the use of platinum drugs in cancer therapy due to their multi-target mode of action. In this context, we report the syntheses of new mononuclear and dinuclear coordination compounds of this element, 1 and 2, derived from the ligand 5-methylsalicylaldehyde 2-furoyl hydrazone (H2L). All three compounds were structurally and spectroscopically characterized, both in the solid state and in solution. In 1, Cu is coordinated by three donor-atoms from the hydrazonic ligand and one chloride ion. H2L is deprotonated at the phenol oxygen. The dinuclear complex 2 is, on the other hand, a dimeric form of 1 in which the chloride ions of a pair of mononuclear units are lost and phenoxo bridges take their places, double-connecting the metal centres and resulting in a single species with the ligand fully deprotonated. The compounds were fairly stable in aqueous medium at room temperature. An experimental-theoretical combined approach demonstrated that all of them are able to bind human serum albumin (HSA), although at different sites and with diverse stoichiometries and affinities (as concluded by the calculated binding energies). In view of this, and due to the well-known antiproliferative activity of hydrazone-containing copper complexes, we consider the compounds presented in here promising, and believe that they deserve more profound studies regarding the assessment of their potential against tumour cell lines.