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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Low-dimensional compounds containing bioactive ligands. Part XIV: High selective antiproliferative activity of tris(5-chloro-8-quinolinolato)gallium (III) complex against human cancer cell lines
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Low-dimensional compounds containing bioactive ligands. Part XIV: High selective antiproliferative activity of tris(5-chloro-8-quinolinolato)gallium (III) complex against human cancer cell lines

机译:含有生物活性配体的低尺寸化合物。 第XIV部分:Tris(5-氯-8-喹啉醇)镓(III)复合物的高选择性抗增殖活性对抗人癌细胞系

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Four gallium(III) complexes, [Ga(ClQ)(3)]center dot MeOH (1 - MeOH), [Ga(ClQ)(3)] (1), [Ga(BrQ)(3)] (2), [Ga(dIQ)(3)] (3) and [Ga(CQ)(3)] (4), were prepared (H-ClQ = 5-chloro-8-quinolinol, H-BrQ = 7-bromo-8-quinolinol, H-dIQ = 5,7-diiodo-8-quinolinol, H-CQ = 5-chloro-7-iodo-8-quinolinol) and characterised by elemental analysis, IR and NMR spectroscopy. Single crystal structure analysis of 1 - MeOH confirmed that the complex has a molecular structure with gallium(III) metal ion coordinated in mer-fashion by N- and O-donor atoms of three ClQ ligands. Stability of all complexes in DMSO was proved by H-1 NMR spectroscopy. The in vitro antiproliferative activity of 1 was evaluated against the A2780, MBA-MB-231 and HCT116 cell lines. Complex 1 displays higher antiproliferative activity (IC50 values in the range 2.1-6 mu m) compared to the ClQ ligand and cisplatin; and a significant selective antiproliferative potency (IC50 = 136 mu m, for normal MRC5pd30 cell line). Radical scavenging experiments revealed that complex 1 exhibits the highest antioxidant activity of the prepared complexes as well as the ligands.
机译:四个镓(III)配合物,[Ga(CLQ)(3)]中心点MeOH(1 - MeOH),[Ga(CLQ)(3)](1),[Ga(BRQ)(3)](2) ,制备[Ga(DIQ)(3)](3)和[Ga(CQ)(3)](4)(H-Clq = 5-氯-8-喹啉醇,H-BRQ = 7-溴 - 8-喹啉醇,H-DIQ = 5,7-二碘-8-喹啉醇,H-CQ = 5-氯-7-Iodo-8-喹啉醇),其特征在于元素分析,IR和NMR光谱。 1 - MeOH的单晶结构分析证实,该复合物具有由三种CLQ配体的N-和O-供体原子配位的镓(III)金属离子的分子结构。通过H-1 NMR光谱证明DMSO中所有复合物的稳定性。对A2780,MBA-MB-231和HCT116细胞系评估1的体外抗增殖活性。与CLQ配体和顺铂相比,复合物1显示出更高的抗增殖活动(2.1-6μm范围内的IC 50值);和具有显着的选择性抗增殖效力(IC50 =136μm,用于正常MRC5PD30细胞系)。自由基清除实验表明,复合物1表现出制备的复合物的最高抗氧化活性以及配体。

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