Effect of electronic and steric properties of 8-substituted quinolines in gold (III) complexes: Synthesis, electrochemistry, stability, interactions and antiproliferative studies
Effect of electronic and steric properties of 8-substituted quinolines in gold (III) complexes: Synthesis, electrochemistry, stability, interactions and antiproliferative studies
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DOI：
10.1016/j.jinorgbio.2017.06.004
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发表时间：
2017-09-01
影响因子：
3.9
通讯作者：
Cabrera, Silvia
中科院分区：
文献类型：
--
作者：
Casado-Sanchez, Antonio;Martin-Santos, Cecilia;Cabrera, Silvia
在这项工作中，新的金（III）与喹啉配体的配合物的合成和表征。这些配合物含有不同的空间和电子性质的给体原子在8-位的喹啉，以调节它们的稳定性和它们的生物活性。它们的氧化还原电位，在有机和水溶剂中的稳定性，以及它们在一组六种不同的人类肿瘤细胞系中的生物活性。此外，配合物与模型生物分子（pBR 322和L-乙酰-N-半胱氨酸）的相互作用研究表明，它们的主要目标是蛋白质。从这些研究中，我们发现，金（III）与N-甲苯磺酰基-8-氨基喹啉配体的配合物是最活跃的复杂的所有肿瘤细胞系，包括顺铂耐药T-47 D和WiDr细胞系。此外，该复合物在DMSO和盐水溶液中显示出最稳定的化合物，甚至在几个小时后也是如此。
In this work the synthesis and characterization of new gold(III) complexes with quinoline ligands are described. These complexes contain different steric and electronic properties of the donor atom at 8-position of the quinoline in order to modulate their stability and their biological activity. Their redox potential, stability in organic and aqueous solvents, and their biological activity in a panel of six different human tumor cell lines are also presented. In addition, interaction studies of the complexes with model biological molecules (pBR322 and Lacetyl-N-cysteine) were carried out, suggesting that their main target are proteins. From these studies, we have found that the gold(III) complex with an N-tosyl-8-aminoquinoline ligand is the most active complex in all the tumor cell lines, including the cisplatin resistant T-47D and WiDr cell lines. Moreover, this complex showed to be the most stable compound in DMSO and saline solution, even after several hours.