首页> 外文OA文献 >Synthesis and Characterization of New Palladium(II) Complexes with Ligands Derived from Furan-2-carbaldehyde and Benzaldehyde Thiosemicarbazone and their in vitro Cytotoxic Activities against Various Human Tumor Cell Lines
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Synthesis and Characterization of New Palladium(II) Complexes with Ligands Derived from Furan-2-carbaldehyde and Benzaldehyde Thiosemicarbazone and their in vitro Cytotoxic Activities against Various Human Tumor Cell Lines

机译:呋喃-2-甲醛和苯甲醛硫半脲配体的新型钯(II)配合物的合成,表征及其对多种人肿瘤细胞系的体外细胞毒活性

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摘要

With the ligands 4-phenyl-1-(furan-2-carbaldehyde)thiosemicarbazone, HTSC1, (1), 4-phenyl-1-(5 -phenyl-furan-2 carbaldehyde)thiosemicarbazone, HTSC2 (2), o-methoxy benzaldehydethiosemicarbazone, HTSC3 (3), and o-cyano-benzaldehydethiosemicarbazone, HTSC4 (4), the correspondingpalladium(II) complexes, Pd(TSC1)2 (5), Pd(TSC2)2 (6), Pd(TSC3)2 (7), and Pd(TSC4)2 (8) were synthesized and characterized by elemental analysis and spectroscopic techniques. The crystal structureof Pd(TSC3)2 (7) was determined by single-crystal X-ray diffraction. Complex 7 shows a squareplanar geometry, where two deprotonated ligands are coordinated to the PdII center through the nitrogenand sulfur atoms in a trans arrangement. In vitro antitumor studies against different human tumor cell lines have revealed that the palladium(II) complexes 5– 8 are more cytotoxic (IC50 valuesin the range of 0.21 – 3.79 µM) than their corresponding ligands (1 – 4) (> 60 µM). These results indicate that the antiproliferative activity is enhanced when thiosemicarbazone ligands are coordinatedto the metal. Among the studied palladium(II) complexes, 8 exhibits high antitumor activity on K562 chronic myelogenous leukemia cells with a low value of the inhibitory concentration (IC50 =0.21 µM).
机译:具有配体4-苯基-1-(呋喃-2-甲醛)硫代半脲,HTSC1,(1),4-苯基-1-(5-苯基呋喃-2甲醛)硫代半脲,HTSC2(2),邻甲氧基苯甲醛硫代半碳酰胺HTSC3(3)和邻氰基苯甲醛硫代半碳酰胺HTSC4(4),相应的钯(II)配合物,Pd(TSC1)2(5),Pd(TSC2)2(6),Pd(TSC3)2( 7)和Pd(TSC4)2(8)合成并通过元素分析和光谱技术表征。通过单晶X射线衍射确定Pd(TSC3)2(7)的晶体结构。配合物7显示出正方形的几何形状,其中两个去质子化的配体通过反式排列的氮和硫原子与PdII中心配位。针对不同人类肿瘤细胞系的体外抗肿瘤研究表明,钯(II)配合物5-8比相应的配体(1-4)(> 60 µM)具有更高的细胞毒性(IC50值在0.21-3.79 µM范围内)。 。这些结果表明,当硫代半脲配体与金属配位时,抗增殖活性增强。在所研究的钯(II)配合物中,有8种对K562慢性粒细胞性白血病细胞表现出高抗肿瘤活性,抑制浓度值低(IC50 = 0.21 µM)。

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