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5,7-二氯-2-甲基-8-羟基喹啉有机金属Ru配合物的抗肿瘤活性研究
Discovery of a high in vitro antitumor activities of organometallic ruthenium(Ⅱ)-arene complexe with 5,7-dichloro-2-methyl-8-quinolinol
【Author】 Ting Meng;Hua-Hong Zou;Zi-Lu Chen;Kai Wang;Fu-Pei Liang;School of Chemistry &Pharmaceutical sciences of Guangxi Normal University;College of Chemistry and Bioengineering, Guilin University of Technology;
【机构】 广西师范大学化学与药学学院; 桂林理工大学化学与生物工程学院;
【摘要】 报道了一种5,7-二氯-2-甲基-8-羟基喹啉有机金属钌配合物[Ru(η6-p-cymene)Cl-(MClClQ)]的合成、结构表征与抗肿瘤活性研究。MTT结果表明该配合物对4种肿瘤细胞均表现出不同程度的增殖抑制作用,总体上表现出比相应的配体强;特别是对HeLa细胞株的IC50值达2.00±0.20 nM,高于相同条件下的8-羟基喹啉衍生物的有机金属钌配合物的活性,而对人体正常肝细胞HL-7702的毒性很小。实验结果表明5,7-二氯-2-甲基-8-羟基喹啉有机金属钌配合物是一种潜在的抗癌药物。
【Abstract】 Herein, we report the synthesis, structure characterization and anti-cancer of a organometallic Ru(Ⅱ)-arene complex [Ru(η6-p-cymene)Cl-(MClClQ)]. MTT assay showed that the complex is more selective for HeLa cell line versus normal HL-7702 cells. In addition, complex having the anti-cancer active H-MClClQ ligand showed remarkable cell cytotoxicity, giving the respective IC50 values of 2.00±0.20 nM on HeLa cancer cells, which was more active than the other 8-hydroxyquinoline derivatives Ru(Ⅱ)-arene complexes. Interestingly, this Ru(Ⅱ)-arene complex was significantly less toxic to HL-7702 normal cells. The experimental results show that 5,7-dichloro-2-methyl-8-hydroxyquinoline organometallic Ru(Ⅱ) complex is a potential anticancer drug.
【Key words】 5,7-dichloro-2-methyl-8-quinolinol; Ru(II) complex; apoptosis;
- 【会议录名称】 中国化学会2019年中西部地区无机化学化工学术研讨会会议论文集
- 【会议名称】中国化学会2019年中西部地区无机化学化工学术研讨会
- 【会议时间】2019-04-19
- 【会议地点】中国重庆
- 【分类号】TQ460.1
- 【主办单位】中国化学会(Chinese Chemical Society)