首页> 外文期刊>Zeitschrift fur Naturforschung, B. A Journal of Chemical Sciences >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:具有呋喃-2-甲醛和苯甲醛硫代半脲的配体的新型钯(II)配合物的合成,表征及其对多种人类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, HTSC', (1), 4-phenyl-1- (5'-phenyl-furan-2-carbaldehyde)thiosemicarbazone, HTSC ~2 (2), o-methoxy-benzaldehydethiosemicarbazone, HTSC_3 (3), and o-cyano-benzaldehydethiosemicarbazone, HTSC~4 (4), the corresponding palladium(II) complexes, Pd(TSC~1)_2 (5), Pd(TSC~2)_2 (6), Pd(TSC~3)_2 (7), and Pd(TSC~4)_2 (8) were synthesized and characterized by elemental analysis and spectroscopic techniques. The crystal structure of Pd(TSC~3)_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 nitrogen and 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 values in 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 coordinated to 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 (IC_(50) = 0.21 μM).
机译:具有配体4-苯基-1-(呋喃-2-甲醛)硫代半碳酸盐,HTSC',(1),4-苯基-1-(5'-苯基呋喃-2-甲醛)硫代半碳酸盐,HTSC〜2(2 ),邻甲氧基-苯甲醛硫代半碳酸盐HTSC_3(3)和邻氰基-苯甲醛硫代半碳酸盐HTSC〜4(4),相应的钯(II)配合物,Pd(TSC〜1)_2(5),Pd(TSC〜合成了2)_2(6),Pd(TSC〜3)_2(7)和Pd(TSC〜4)_2(8),并通过元素分析和光谱技术对其进行了表征。通过单晶X射线衍射确定Pd(TSC〜3)_2(7)的晶体结构。配合物7显示出正方形平面的几何形状,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比其相应的配体(1-4)(> 60μM)具有更高的细胞毒性(IC50值在0.21-3.79μM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。在研究的钯(II)配合物中,有8种对K562慢性骨髓性白血病细胞表现出高抗肿瘤活性,抑制浓度值低(IC_(50)= 0.21μM)。

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