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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.
Bioinorganic Chemistry and Applications ( IF 4.7 ) Pub Date : 2009-01-08 , DOI: 10.1155/2008/690952
Wilfredo Hernándeza 1 , Juan Paz , Abraham Vaisberg , Evgenia Spodine , Rainer Richter , Lothar Beyer
Affiliation  

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) [HL(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) [HL(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 microM. 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 microM) than the other tested palladium (II) complexes.

中文翻译:

苯甲醛缩氨基硫脲衍生物及其钯 (II) 和铂 (II) 复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。

合成了苯甲醛缩氨基硫脲衍生物的钯 (II) 双螯合 Pd (L(1-3))(2) 和铂 (II) 四核 Pt(4)(L(4))(4) 络合物,并对其进行了表征通过元素分析和 IR、FAB(+)-mass 和 NMR ((1)H, (13)C) 光谱。复合物 Pd(L(2))(2) [HL(2) = m-CN-苯缩氨基硫脲] 显示方形平面几何形状,其中两个去质子化配体 (L) 通过氮和硫原子与 Pd(II) 配位在转排中,复合物 Pt(4)(L(4))(4) [HL(4) = 4-phenyl-1-benzaldehyde thiosemicarbazone] 具有四核几何结构,四个三齿配体与四个 Pt(II) 配位离子通过碳(芳环)、氮和硫原子,其中配体在 NH 基团处去质子化。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测定表明,钯 (II) 和铂 (II) 配合物比它们的配体更具细胞毒性,IC(50) 值范围为0.07-3.67 微米。四核复合物 Pt(4)(L(4))(4) 在配体的末端胺基中带有苯基,显示出比其他测试钯更高的抗增殖活性(CI(50) = 0.07-0.12 microM)( II) 复合物。
更新日期:2019-11-01
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