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含三唑基葡萄糖配体的 Pt(II) 配合物的平面正方形与三角双锥几何构型作为潜在的抗癌剂。

Square-Planar vs. Trigonal Bipyramidal Geometry in Pt(II) Complexes Containing Triazole-Based Glucose Ligands as Potential Anticancer Agents.

机构信息

Dipartimento di Scienze Chimiche, Università di Napoli Federico II, Complesso Universitario di Monte S. Angelo, Via Cintia 21, 80126 Napoli, Italy.

出版信息

Int J Mol Sci. 2021 Aug 13;22(16):8704. doi: 10.3390/ijms22168704.

Abstract

This article describes the synthesis, characterization, and biological activity of novel square-planar cationic platinum(II) complexes containing glucoconjugated triazole ligands and a comparison with the results obtained from the corresponding five-coordinate complexes bearing the same triazole ligands. Stability in solution, reactivity with DNA and small molecules of the new compounds were evaluated by NMR, fluorescence, and UV-vis absorption spectroscopy, together with their cytotoxic action against pairs of immortalized and tumorigenic cell lines. The results show that the square-planar species exhibit greater stability than the corresponding five-coordinate ones. Furthermore, although the square-planar complexes are less cytotoxic than the latter ones, they exhibit a certain selectivity. These results simultaneously demonstrate that overall stability is a fundamental prerequisite for preserving the performance of the agents and that coordinative saturation constitutes a point in favor of their biological action.

摘要

本文描述了新型方平面阳离子铂(II)配合物的合成、表征和生物活性,这些配合物含有葡萄糖结合的三唑配体,并与具有相同三唑配体的相应五配位配合物的结果进行了比较。通过 NMR、荧光和紫外可见吸收光谱评估了新化合物在溶液中的稳定性、与 DNA 和小分子的反应活性,以及它们对成对的永生化和致瘤细胞系的细胞毒性作用。结果表明,方平面物种比相应的五配位物种具有更高的稳定性。此外,尽管方平面配合物的细胞毒性比后者低,但它们具有一定的选择性。这些结果同时表明,整体稳定性是保持试剂性能的基本前提,而配位饱和则有利于它们的生物作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ed89/8395886/249bc8f5cd54/ijms-22-08704-g001.jpg

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