Dipartimento di Scienze Chimiche, Università di Napoli Federico II, Complesso Universitario di Monte S. Angelo, Via Cintia 21, 80126 Napoli, Italy.
Int J Mol Sci. 2021 Aug 13;22(16):8704. doi: 10.3390/ijms22168704.
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.
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。
