Canudo-Barreras Guillermo, Ortego Lourdes, Izaga Anabel, Marzo Isabel, Herrera Raquel P, Gimeno M Concepción
Departamento de Química Inorgánica, Instituto de Síntesis Química y Catálisis Homogénea (ISQCH), CSIC-Universidad de Zaragoza, C/Pedro Cerbuna 12, 50009 Zaragoza, Spain.
Laboratorio de Organocatálisis Asimétrica, Departamento de Química Orgánica, Instituto de Síntesis Química y Catálisis Homogénea (ISQCH), CSIC-Universidad de Zaragoza, C/Pedro Cerbuna 12, 50009 Zaragoza, Spain.
Molecules. 2021 Nov 16;26(22):6891. doi: 10.3390/molecules26226891.
In this work, two thiourea ligands bearing a phosphine group in one arm and in the other a phenyl group () or 3,5-di-CF substituted phenyl ring () have been prepared and their coordination to Au and Ag has been studied. A different behavior is observed for gold complexes, a linear geometry with coordination only to the phosphorus atom or an equilibrium between the linear and three-coordinated species is present, whereas for silver complexes the coordination of the ligand as P^S chelate is found. The thiourea ligands and their complexes were explored against different cancer cell lines (HeLa, A549, and Jurkat). The thiourea ligands do not exhibit relevant cytotoxicity in the tested cell lines and the coordination of a metal triggers excellent cytotoxic values in all cases. In general, data showed that gold complexes are more cytotoxic than the silver compounds with , in particular the complexes [Au(PPh)]OTf, the bis(thiourea) [Au()]OTf and the gold-thiolate species [Au(SR)]. In contrast, with better results are obtained with silver species [Ag(PPh)]OTf and the [Ag()]OTf. The role played by the ancillary ligand bound to the metal is important since it strongly affects the cytotoxic activity, being the bis(thiourea) complex the most active species. This study demonstrates that metal complexes derived from thiourea can be biologically active and these compounds are promising leads for further development as potential anticancer agents.
在本工作中，制备了两种硫脲配体，一种配体的一条臂上带有膦基，另一条臂上带有苯基（）或3,5 - 二 - 三氟甲基取代的苯环（），并研究了它们与金和银的配位情况。对于金配合物，观察到了不同的行为，存在仅与磷原子配位的线性几何结构，或者线性和三配位物种之间的平衡，而对于银配合物，发现配体以P^S螯合物形式配位。研究了硫脲配体及其配合物对不同癌细胞系（HeLa、A549和Jurkat）的作用。硫脲配体在测试的细胞系中未表现出显著的细胞毒性，而金属配位在所有情况下都引发了优异的细胞毒性值。总体而言，数据表明金配合物比银化合物更具细胞毒性，尤其是配合物[Au(PPh)]OTf、双（硫脲）[Au()]OTf和金硫醇盐物种[Au(SR)]。相比之下，银物种[Ag(PPh)]OTf和[Ag()]OTf取得了更好的结果。与金属结合的辅助配体所起的作用很重要，因为它强烈影响细胞毒性活性，双（硫脲）配合物是最具活性的物种。这项研究表明，源自硫脲的金属配合物可能具有生物活性，并且这些化合物作为潜在的抗癌药物有进一步开发的前景。
