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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, characterization and biological activity of Pt(II) and Pt(IV) complexes with 5-methyl-5(4-pyridyl)-2,4-imidazolidenedione.
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Synthesis, characterization and biological activity of Pt(II) and Pt(IV) complexes with 5-methyl-5(4-pyridyl)-2,4-imidazolidenedione.

机译:Pt(II)和Pt(IV)与5-甲基-5(4-吡啶基)-2,4-咪唑啉二酮的配合物的合成,表征和生物学活性。

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摘要

New platinum(II) and platinum(IV) complexes with 5-methyl-5(4-pyridyl)-2,4-imidazolidenedione and various halogen ions with general formula [PtL(2)X(2)] and [PtL(2)Cl(4)], where L is the organic ligand and X is Cl(-), Br(-), J(-), were synthesized. The molecular formulae of all the complexes were confirmed by elemental analysis, IR, (1)H, (13)C NMR spectral analyses and molar conductivity. The cytotoxic effects of these complexes were examined on some human tumor cell lines. The newly synthesized cis-[PtL(2)Cl(2)] exerted cytotoxic activity against SKW-3, MCF-7, EJ, U-266 tumor cell lines, while cis-[PtL(2)Br(2)], trans-[PtL(2)I(2)] were less active. The higher oxidation state complex cis-[PtL(2)Cl(4)] was inactive in all cell lines but in SKW-3 some augmentation of the cytotoxicity was seen after co-administration of ascorbic acid but not when treated in combination with reduced glutathione or N-acetylcysteine. A DNA-fragmentation analysis revealed that the cytotoxicity of the dichloro analogue, characterized with superior activity compared to the other complexes, is mediated by induction of apoptotic cell death.
机译:新的铂(II)和铂(IV)与5-甲基-5(4-吡啶基)-2,4-咪唑啉二酮和各种卤素离子的配合物,通式为[PtL(2)X(2)]和[PtL(2) )Cl(4)],其中L为有机配体,X为Cl(-),Br(-),J(-)。通过元素分析,IR,(1)H,(13)C NMR光谱分析和摩尔电导率确定所有配合物的分子式。检查了这些复合物对某些人类肿瘤细胞系的细胞毒性作用。新合成的顺式[[PtL(2)Cl(2)]对SKW-3,MCF-7,EJ,U-266肿瘤细胞系具有细胞毒活性,而顺式[[PtL(2)Br(2)],反式[PtL(2)I(2)]的活性较低。较高氧化态的复合物顺式[[PtL(2)Cl(4)]在所有细胞系中均无活性,但在SKW-3中,抗坏血酸并用后细胞毒性增加,但与降低剂量联合使用时则无谷胱甘肽或N-乙酰半胱氨酸。 DNA片段分析表明,与其他复合物相比,具有更高活性的二氯类似物的细胞毒性是通过诱导凋亡性细胞死亡来介导的。

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