Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Ministry of Education China, School of Chemistry & Chemical Engineering of Guangxi Normal University, Guilin 541004, PR China.
Dalton Trans. 2011 Feb 28;40(8):1684-92. doi: 10.1039/c0dt01310b. Epub 2011 Jan 24.
Three new lanthanide complexes with dihalo-substituted 8-quinolinol: [Gd(BrQ)(3)(H(2)O)(2)]·1.33EtOH·0.33H(2)O (1), [Dy(ClQ)(3)(H(2)O)(2)]·1.33EtOH·0.33H(2)O (2), [Er(ClQ)(3)(H(2)O)(2)]·1.33EtOH·0.33H(2)O (3) (H-BrQ = 5,7-dibromo-8-quinolinol, H-ClQ = 5,7-dichloro-8-quinolinol) have been synthesized and characterized by elemental analysis, IR, ESI-MS, single-crystal X-ray diffraction and TGA. The single-crystal X-ray diffraction analyses reveal that complexes 1-3 are mononuclear and isostructural. Each metal centre is coordinated by three dihalo-substituted 8-quinolinol and two aqua ligands. The in vitro cytotoxicity of dihalo-substituted 8-quinolinol and complexes 1-3 against liver cancer BEL7404 was evaluated. The IC(50) values of 1-3 to BEL7404 were 47.2 ± 2.6, 18.3 ± 1.0 and 31.5 ± 1.2 nM, respectively. The lanthanide complexes 1-3 exhibited significantly enhanced cytotoxicity vs. free substituted 8-quinolinol. The binding properties of dihalo-substituted 8-quinolinol and complexes 1 and 2 to DNA were investigated by UV-vis, fluorescence, CD spectroscopy and viscosity measurements, as well as agarose gel electrophoresis experiments. Both complexes 1 and 2 interact more strongly with DNA than the free quinolinol ligand. Intercalation is the most probable binding mode for both the complexes and the quinolinol ligands.
三种新型镧系元素配合物与二卤代取代 8-喹啉醇：[Gd(BrQ)(3)(H2O)(2)]·1.33EtOH·0.33H2O(1)，[Dy(ClQ)(3)(H2O)(2)]·1.33EtOH·0.33H2O(2)，[Er(ClQ)(3)(H2O)(2)]·1.33EtOH·0.33H2O(3)(H-BrQ=5,7-二溴-8-喹啉醇，H-ClQ=5,7-二氯-8-喹啉醇)已被合成并通过元素分析、IR、ESI-MS、单晶 X 射线衍射和 TGA 进行了表征。单晶 X 射线衍射分析表明，配合物 1-3 为单核且同构。每个金属中心由三个二卤代取代 8-喹啉醇和两个水配体配位。评估了二卤代取代 8-喹啉醇和配合物 1-3 对肝癌 BEL7404 的体外细胞毒性。1-3 对 BEL7404 的 IC50 值分别为 47.2±2.6、18.3±1.0 和 31.5±1.2 nM。镧系元素配合物 1-3 对游离取代 8-喹啉醇表现出显著增强的细胞毒性。通过紫外可见、荧光、CD 光谱和粘度测量以及琼脂糖凝胶电泳实验研究了二卤代取代 8-喹啉醇和配合物 1 和 2 与 DNA 的结合性质。配合物 1 和 2 与 DNA 的相互作用均强于游离喹啉醇配体。对于两种配合物和喹啉醇配体，嵌入都是最可能的结合模式。
