Synthesis and Evaluation of the Cytotoxic Activity of Water-Soluble Cationic Organometallic Complexes of the Type [Pt(η1-C2H4OMe)(L)(Phen)]+ (L = NH3, DMSO; Phen = 1,10-Phenanthroline)
作者:Federica De Castro、Erika Stefàno、Danilo Migoni、Giorgia N. Iaconisi、Antonella Muscella、Santo Marsigliante、Michele Benedetti、Francesco P. Fanizzi
DOI:10.3390/pharmaceutics13050642
日期:——
[PtCl(η1-C2H4OMe)(phen)] (phen = 1,10-phenanthroline, 1) platinum(II) precursor, we synthesized and characterized by multinuclear NMR new [Pt(η1-C2H4OMe)(L)(phen)]+ (L = NH3, 2; DMSO, 3) complexes. These organometallic species, potentially able to interact with cell membrane organic cation transporters (OCT), violating some of the classical rules for antitumor activity of cisplatin analogues, were evaluated for
以[PtCl(η 1 -C 2 H 4 OMe)(phen)] (phen = 1,10-菲咯啉, 1 )铂(II)前体为原料,我们合成了新的[Pt(η 1 - C 2 H 4 OMe)(L)(phen)] + (L = NH 3 , 2 ; DMSO, 3 ) 络合物。这些有机金属物质可能与细胞膜有机阳离子转运蛋白(OCT)相互作用,违反了顺铂类似物抗肿瘤活性的一些经典规则,对其细胞毒性进行了评估。有趣的是,尽管复合物2和3在选定的肿瘤细胞系中比顺铂产生了更大的细胞摄取,但只有3 种表现出相当或更高的抗肿瘤活性。复合物2在测试细胞系(SH-SY5Y、SK-OV-3、Hep-G2、Caco-2、HeLa、MCF-7、MG-63、ZL-65)中的总体低细胞毒性似乎取决于其稳定性通过 NMR 监测评估,在中性水中发生溶剂分解。不同的是,[Pt(η 1 -C 2 H 4 OMe)(DMSO)(phen)]