Department of Chemistry, National Institute of Technology, Rourkela, Odisha 769008, India.
Department of Chemical Engineering, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835215, India.
ACS Appl Bio Mater. 2023 Dec 18;6(12):5360-5371. doi: 10.1021/acsabm.3c00629. Epub 2023 Nov 29.
In this work, three titanium(IV) [Ti(L)] (-) complexes have been reported using three different tridentate dibasic ONO donor hydrazone ligands, pyridine-4-carboxylic acid (3-ethoxy-2-hydroxybenzylidene)-hydrazide (HL), furan-2-carboxylic acid (3-ethoxy-2-hydroxybenzylidene)-hydrazide (HL), and thiophene-2-carboxylic acid (3-ethoxy-2-hydroxybenzylidene)-hydrazide (HL) tethered with heterocyclic moieties. Elemental analysis, FT-IR, UV-vis, NMR, HR-ESI-MS, and single-crystal X-ray analysis have been used to characterize HL and -. In solid structures of -, two ligand molecules with NO donor sets give distorted octahedral geometries to the metal center. The aqueous stability of - was investigated and well correlated to their perceived pharmacological results. During the investigation, all three complexes were found to be hydrolytically stable in a 90% DMSO-/10% DO (v/v) medium up to 48 h. Furthermore, the interaction of - with bovine serum albumin (BSA) was tested using fluorescence and absorption techniques. The complexes showed static quenching with a biomolecular quenching constant of ∼ 10 proposing a high affinity of complexes for BSA. Finally, the anticancer potential of - was tested against HeLa, A549, and NIH-3T3 cell lines. Among all, with an IC value of 11.6 ± 1.1 μM against HeLa cells was found to be the most cytotoxic in the series. Furthermore, it has been found that the compounds induce an apoptotic mode of cell death, which is confirmed by the live cell confocal microscopy and flow cytometry techniques.
在这项工作中，报道了三种使用三种不同的三齿双基 ONO 供体腙配体的钛(IV)Ti(L)配合物，吡啶-4-羧酸(3-乙氧基-2-羟基苯亚甲基)-腙（HL）、呋喃-2-羧酸(3-乙氧基-2-羟基苯亚甲基)-腙（HL）和噻吩-2-羧酸(3-乙氧基-2-羟基苯亚甲基)-腙（HL）与杂环部分连接。使用元素分析、FT-IR、UV-vis、NMR、HR-ESI-MS 和单晶 X 射线分析对 HL 和-进行了表征。在-的固体结构中，两个具有 NO 供体的配体分子为金属中心提供了扭曲的八面体几何构型。研究了-的水稳定性，并与预期的药理学结果很好地相关。在研究过程中，发现所有三种配合物在 90% DMSO-/10% DO（v/v）介质中 48 小时内都具有水解稳定性。此外，还使用荧光和吸收技术测试了-与牛血清白蛋白（BSA）的相互作用。该复合物显示出静态猝灭，生物分子猝灭常数为 ∼ 10，表明复合物与 BSA 具有高亲和力。最后，测试了-对 HeLa、A549 和 NIH-3T3 细胞系的抗癌潜力。在所有化合物中，对 HeLa 细胞的 IC 值为 11.6±1.1 μM 的 被发现具有最高的细胞毒性。此外，还发现化合物诱导细胞凋亡死亡模式，这通过活细胞共聚焦显微镜和流式细胞术技术得到证实。
