首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Stereospecific ligands and their complexes. Part VII. Synthesis, characterization and in vitro antitumoral activity of platinum(II) complexes with O,O'-dialkyl esters of (S,S)-ethylenediamine-N,N'-di-2-(4-methyl)pentanoic acid.
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Stereospecific ligands and their complexes. Part VII. Synthesis, characterization and in vitro antitumoral activity of platinum(II) complexes with O,O'-dialkyl esters of (S,S)-ethylenediamine-N,N'-di-2-(4-methyl)pentanoic acid.

机译:立体特异性配体及其复合物。第七部分铂(II)与(S,S)-乙二胺-N,N'-二-2-(4-甲基)戊酸的O,O'-二烷基酯的配合物的合成,表征和体外抗肿瘤活性。

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摘要

Platinum(II) complexes (1-4) with bidentate N,N'-ligands, O,O'-dialkyl esters (alkyl = ethyl, n-propyl, n-butyl and n-pentyl), of (S,S)-ethylenediamine-N,N'-di-2-(4-methyl)pentanoic acid were synthesized and characterized by IR, (1)H NMR and (13)C NMR spectroscopy and elemental analysis. DFT calculations were performed for the complexes and it was found that only one diastereoisomer could be formed. Cytotoxic activity of complexes 1-4 was determined against chronic lymphocytic leukemia cells (CLL) and compared to the activity of ligand precursors L1 . 2HCl-L4.2HCl and corresponding palladium(II) complexes, [PdCl(2)L] (L = L1-L4). The complexes were found to exhibit significantly higher antitumor activities than cisplatin on CLL cells. Cytotoxic effect of platinum(II) complexes on CLL cells was higher compared to corresponding palladium(II) complexes. In addition the mode of cell death induced by platinum(II) complexes was determined.
机译:具有(S,S)的二齿N,N'-配体,O,O'-二烷基酯(烷基=乙基,正丙基,正丁基和正戊基)的铂(II)配合物(1-4)合成了乙撑二胺-N,N'-二-2-(4-甲基)戊酸,并通过IR,(1)H NMR和(13)C NMR光谱及元素分析对其进行了表征。对复合物进行了DFT计算,发现只能形成一种非对映异构体。确定复合物1-4对慢性淋巴细胞白血病细胞(CLL)的细胞毒活性,并将其与配体前体L1的活性进行比较。 2HCl-L4.2HCl和相应的钯(II)配合物[PdCl(2)L](L = L1-L4)。发现该复合物在CLL细胞上显示出比顺铂明显更高的抗肿瘤活性。与相应的钯(II)复合物相比,铂(II)复合物对CLL细胞的细胞毒性作用更高。另外,测定了由铂(II)配合物诱导的细胞死亡的模式。

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