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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:苯甲醛硫杂氨基脲类衍生物及其钯(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

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摘要

The palladium (II) bis-chelate Pd (L1−3)2 and platinum (II) tetranuclear Pt4(L4)4 complexes of benzaldehyde thiosemicarbazone derivatives have been synthesized, and characterized by elemental analysis and IR, FAB(+)-mass and NMR (1H, 13C) spectroscopy. The complex Pd(L2)2 [HL2 = m-CN-benzaldehyde thiosemicarbazone] shows a square-planar geometry with two deprotonated ligands (L) coordinated to PdII through the nitrogen and sulphur atoms in a transarrangement, while the complex Pt4(L4)4 [HL4 = 4-phenyl-1-benzaldehyde thiosemicarbazone] has a tetranuclear geometry with four tridentate ligands coordinated to four PtII 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 IC50 values at the range of 0.07–3.67 μM. The tetranuclear complex Pt4(L4)4, with the phenyl group in the terminal amine of the ligand, showed higher antiproliferative activity (CI50 = 0.07–0.12 μM) than the other tested palladium (II) complexes.
机译:合成了苯甲醛硫半碳carb衍生物的钯(II)双螯合物Pd(L 1-3 )2和铂(II)四核Pt4(L 4 )4配合物,并通过元素分析和IR,FAB(+)-质量和NMR( 1 H, 13 C)光谱进行表征。复杂的Pd(L 2 )2 [HL 2 = m-CN-苯甲醛硫代半碳酮]呈方形平面几何结构,带有两个去质子化的配体(L)与Pd < sup> II 通过氮和硫原子进行重排,而复合物Pt4(L 4 )4 [HL 4 = 4-苯基-1-苯甲醛硫半碳酸盐]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,其中配体在NH基团上被去质子化。测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,IC50值在0.07–3.67范围内微米具有配体末端胺的苯基的四核复合物Pt4(L 4 )4具有比其他测试的钯(II)配合物更高的抗增殖活性(CI50 = 0.07–0.12μM) 。

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