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钯(II)配合物与 R(2)edda 衍生配体。第四部分。(S,S)-乙二胺-N,N'-二-2-(4-甲基)-戊二酸二盐酸盐的 O,O'-二烷基酯及其钯(II)配合物:合成、表征及对慢性淋巴细胞白血病 (CLL)细胞的体外抗肿瘤活性。

Palladium(II) complexes with R(2)edda derived ligands. Part IV. O,O'-dialkyl esters of (S,S)-ethylenediamine-N,N'-di-2-(4-methyl)-pentanoic acid dihydrochloride and their palladium(II) complexes: synthesis, characterization and in vitro antitumoral activity against chronic lymphocytic leukemia (CLL) cells.

机构信息

Department of Chemistry, Faculty of Science, University of Kragujevac, R. Domanovića 12, 34000 Kragujevac, Serbia.

出版信息

Eur J Med Chem. 2010 Sep;45(9):3601-6. doi: 10.1016/j.ejmech.2010.05.005. Epub 2010 May 12.

Abstract

Four novel bidentate N,N'-ligand precursors, including O,O'-dialkyl esters (alkyl = ethyl, n-propyl, n-butyl and n-pentyl), L1 x 2 HCl-L4 x 2 HCl, of (S,S)-ethylenediamine-N,N'-di-2-(4-methyl)-pentanoic acid dihydrochloride [(S,S)-H(4)eddl]Cl(2) and the corresponding palladium(II) complexes 1-4, were prepared and characterized by IR, (1)H NMR and (13)C NMR spectroscopy and elemental analysis. In vitro cytotoxicity of all compounds was determined against chronic lymphocytic leukemia cells (CLL). The compounds were found to exhibit higher antitumoral activity than cisplatin. The most active compound 2, [PdCl(2){(S,S)-nPr(2)eddl}], was found to be 13.6 times more active than cisplatin on CLL cells.

摘要

四种新型双齿 N,N'-配体前体,包括 O,O'-二烷基酯(烷基=乙基、正丙基、正丁基和正戊基)、L1 x 2 HCl-L4 x 2 HCl、(S,S)-乙二胺-N,N'-二-2-(4-甲基)戊二酸二盐酸盐[(S,S)-H(4)eddl]Cl(2)和相应的钯(II)配合物 1-4,通过 IR、(1)H NMR 和(13)C NMR 光谱和元素分析进行了制备和表征。所有化合物的体外细胞毒性均针对慢性淋巴细胞白血病细胞(CLL)进行了测定。结果发现,这些化合物比顺铂具有更高的抗肿瘤活性。最活跃的化合物 2,[PdCl(2){(S,S)-nPr(2)eddl}],对 CLL 细胞的活性比顺铂高 13.6 倍。

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