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Synthesis, characterization, and in vitro cytotoxic activities of benzaldehyde thiosemicarbazone derivatives and their palladium(II) and platinum(II) complexes against various human tumor cell lines

机译:苯甲醛硫代半碳酰胺衍生物及其钯(II)和铂(II)配合物对各种人类肿瘤细胞系的合成,表征和体外细胞毒活性

摘要

The palladium (II) bis-chelate Pd (L 1 - 3) 2 and platinum (II) tetranuclear Pt 4 (L 4) 4 complexes of benzaldehyde thiosemicarbazone derivatives have been synthesized, and characterized by elemental analysis and IR, FAB (+) -mass and NMR (1 H, 13 C) spectroscopy. The complex Pd (L 2) 2 [H L 2 = m -CN-benzaldehyde thiosemicarbazone] shows a square-planar geometry with two deprotonated ligands (L) coordinated to Pd II through the nitrogen and sulphur atoms in a transarrangement, while the complex Pt 4 (L 4) 4 [H L 4 = 4 -phenyl-1-benzaldehyde thiosemicarbazone] has a tetranuclear geometry with four tridentate ligands coordinated to four Pt II ions through the carbon (aromatic ring), nitrogen, and sulphur atoms where the ligands are deprotonated at the NH group. The in vitro antitumor activity of the ligands and their complexes was determined against different human tumor cell lines, which revealed that the palladium (II) and platinum (II) complexes are more cytotoxic than their ligands with IC 50 values at the range of 0.07-3.67 µM. The tetranuclear complex Pt 4 (L 4) 4, with the phenyl group in the terminal amine of the ligand, showed higher antiproliferative activity (CI 50 = 0.07-0.12 µM) than the other tested palladium (II) complexes.
机译:已合成了苯甲醛硫代半碳a酮衍生物的钯(II)双螯合物Pd(L 1-3)2和铂(II)四核Pt 4(L 4)4配合物,并通过元素分析和IR,FAB(+)进行了表征-质谱和NMR(1 H,13 C)光谱。复杂的Pd(L 2)2 [HL 2 =间-CN-苯甲醛硫代半碳酸盐]显示方形平面的几何结构,其中两个去质子化的配体(L)通过氮和硫原子以换位方式与Pd II配位,而复杂的Pt 4(L 4)4 [HL 4 = 4-苯基-1-苯甲醛硫代半碳酸盐]具有四核几何形状,具有四个三齿配体,通过碳(芳环),氮和硫原子与四个Pt II离子配位,配体为NH组去质子化确定了配体及其配合物对不同人类肿瘤细胞系的体外抗肿瘤活性,这表明钯(II)和铂(II)配合物比其配体更具细胞毒性,IC 50值为0.07- 3.67 µM。具有配体末端胺中的苯基的四核配合物Pt 4(L 4)4显示出比其他测试的钯(II)配合物更高的抗增殖活性(CI 50 = 0.07-0.12 µM)。

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