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首页> 外文期刊>Journal of Inorganic Biochemistry: An Interdisciplinary Journal >The 1,3-diaryltriazenido(p-cymene)ruthenium(II) complexes with a high in vitro anticancer activity
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The 1,3-diaryltriazenido(p-cymene)ruthenium(II) complexes with a high in vitro anticancer activity

机译：具有高体外抗癌活性的1,3-二芳基三氮杂ido（对甲基cy）钌（II）配合物

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1,3-Diatyltriazenes (1) were let to react with [RuCl2(p-cymene)](2) in the presence of trimethylamine to give neutral 1,3-diatyltriazenido(p-cymene)ruthenium(11) complexes, [RuCl(p-cymene)(ArNNNAr)] (2). The molecular composition of the products 2 was confirmed by NMR spectroscopy and mass spectrometry. The structures of the selected complexes were confirmed by a single crystal X-ray analysis. All triazenido-ruthenium complexes were highly cytotoxic against human cervical carcinoma HeLa cells with IC50 below 6 mu M, as determined by a spectrophotometric MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide) method. The most active was [RuCl(p-cymene)(ArNNNAr)] (Ar = 4-Cl-3-(CF3)-C6H3) (2g) with IC50 of 0.103 +/- 0.006 mu M. In comparison with the data for the non-coordinated triazenes 1, the triazenido-ruthenium complexes 2 exhibited up to 560-times higher activity. Three selected complexes were highly cytotoxic also against several tumor cell lines: laryngeal carcinoma HEp-2 cells and their drug-resistant HEp-2 subline (7 T), colorectal carcinoma HCT-116 cells, lung adenocarcinoma H460 cells, and mammary carcinoma MDA-MB-435 cells. The compounds 2g and [RuCl(p-cymene)(ArNNNAr)] (Ar = 4-I-C6H4) (2j) were similarly cytotoxic against parental and drug-resistant cells. Time and dose dependent accumulation of the cells in the S phase of the cell cycle was induced by the compound 2g, triggering apoptosis. Our preliminary results indicate triazenido-ruthenium complexes as promising anticancer drug candidates. (C) 2015 Elsevier Inc. All rights reserved.
机译：在三甲胺的存在下，使1,3-二脂基三氮烯（1）与[RuCl2（p-cymene）]（2）反应，得到中性1,3-二乙酰基三氮杂（p-cymene）钌（11）络合物[RuCl （p-cymene）（ArNNNAr）]（2）。产物2的分子组成通过NMR光谱法和质谱法确认。所选配合物的结构通过单晶X射线分析确认。分光光度法MTT（3-（4,5-二甲基噻唑-2-基）-2,5-二苯基溴化四氮唑）测定，所有三氮杂ido-钌络合物对人宫颈癌HeLa细胞具有高度细胞毒性，IC50低于6μM ） 方法。活性最高的是[RuCl（p-cymene）（ArNNNAr）]（Ar = 4-Cl-3-（CF3）-C6H3）（2g），IC50为0.103 +/- 0.006μM。非配位的三氮烯1，三叠氮基-钌络合物2的活性提高了560倍。三种选定的复合物对多种肿瘤细胞系也具有高度的细胞毒性：喉癌HEp-2细胞及其耐药性HEp-2亚系（7 T），结直肠癌HCT-116细胞，肺腺癌H460细胞和乳腺癌MDA- MB-435细胞。化合物2g和[RuCl（p-cymene）（ArNNNAr）]（Ar = 4-I-C6H4）（2j）对亲本和耐药细胞具有类似的细胞毒性。化合物2g诱导细胞周期S期中细胞的时间和剂量依赖性积累，触发细胞凋亡。我们的初步结果表明三氮杂ido-钌配合物是有前途的抗癌药物候选物。 （C）2015 Elsevier Inc.保留所有权利。

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