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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >1-(2-Picolyl)-substituted 1,2,3-triazole as novel chelating ligand for the preparation of ruthenium complexes with potential anticancer activity
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1-(2-Picolyl)-substituted 1,2,3-triazole as novel chelating ligand for the preparation of ruthenium complexes with potential anticancer activity

机译：1-（2-Picolyl）-取代的1,2,3-三唑作为新型螯合配体，用于制备具有潜在抗癌活性的钌配合物

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摘要

The 1,4-disubstituted 1,2,3-triazole ligand prepared by click chemistry 1-(2-picolyl)-4-phenyl-1H-1,2,3-triazole (ppt) was investigated as novel chelating ligand for Ru(ii) complexes with potential antitumor activity. The preparation and structural characterization, mainly by NMR spectroscopy in solution and by X-Ray crystallography in the solid state, of four new Ru(ii) complexes is reported: two isomeric Ru-dmso compounds, trans,cis-[RuCl _2(dmso-S)_2(ppt)] (1) and cis,cis-[RuCl_2(dmso-S) _2(ppt)] (2), and two half-sandwich Ru-[9]aneS_3 coordination compounds, [Ru([9]aneS_3)(dmso-S)(ppt)][CF _3SO_3]_2 (3) and [Ru([9]aneS_3)Cl(ppt)] [CF_3SO_3] (4). In all compounds ppt firmly binds to ruthenium in a bidentate fashion through the pyridyl nitrogen atom and the triazole N2, thus forming a puckered six-membered ring. The chemical behavior in aqueous solution of the water-soluble complexes 3 and 4 was studied by UV-Vis and NMR spectroscopy and compared to that of the previously described organometallic analogue [Ru(η6-p-cymene)Cl(ppt)][Cl] (5) in view of their potential antitumor activity. Compounds 3-5 were tested also in vitro for cytotoxic activity against two human cancer cell lines, one sensitive and one resistant to cisplatin, in comparison with cisplatin. Compound 4, the one that aquates faster, was found to be more cytotoxic than cisplatin against human lung squamose carcinoma cell line (A-549).
机译：通过点击化学1-（2-picolyl）-4-苯基-1H-1,2,3-三唑（ppt）制备的1,4-二取代1,2,3-三唑配体被研究为Ru的新型螯合配体（ii）具有潜在抗肿瘤活性的复合物。报道了四种新的Ru（ii）配合物的制备和结构表征，主要是通过溶液中的NMR光谱和固态的X射线晶体学：两种异构的Ru-dmso化合物，反式，顺式-[RuCl _2（dmso） -S）_2（ppt）]（1）和cis，cis- [RuCl_2（dmso-S）_2（ppt）]（2）和两个半三明治Ru- [9] aneS_3配位化合物[Ru（[ 9] aneS_3）（dmso-S）（ppt）] [CF _3SO_3] _2（3）和[Ru（[9] aneS_3）Cl（ppt）] [CF_3SO_3]（4）。在所有化合物中，ppt通过吡啶基氮原子和三唑N2以二齿形式牢固地与钌结合，从而形成折叠的六元环。通过UV-Vis和NMR光谱研究了水溶性配合物3和4在水溶液中的化学行为，并将其与先前描述的有机金属类似物[Ru（η6-p-cymene）Cl（ppt）] [Cl ]（5）鉴于其潜在的抗肿瘤活性。与顺铂相比，还体外测试了化合物3-5对两种人癌细胞系的细胞毒性活性，一种对顺铂敏感，一种对顺铂耐药。发现化合物4（水合速度更快）对人肺鳞癌癌细胞系（A-549）的毒性比顺铂强。

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