Design, Synthesis and Biological Evaluation of Palladium (II) Complexes with 1-(substituted benzyl) azetidine-3,3-dicarboxylates as Leaving Group

被引:0
作者
Xu, Gang [1 ,2 ]
Lu, Hua [1 ,2 ]
Jiang Zhitao [1 ,2 ]
Zhang, Shuying [1 ]
Gou, Shaohua [1 ,2 ]
机构
[1] Southeast Univ, Sch Chem & Chem Engn, Pharmaceut Res Ctr, Nanjing 211189, Jiangsu, Peoples R China
[2] Southeast Univ, Jiangsu Prov Hitech Key Lab Biomed Res, Nanjing 211189, Jiangsu, Peoples R China
基金
中国国家自然科学基金;
关键词
Antitumor activity; palladium (II) complex; DNA interaction; 2; '-bipyridine; 1-(substituted benzyl) azetidine; 3,3-dicarboxylates; agarose gel electrophoresis; DNA-BINDING; PLATINUM(II) COMPLEXES; 2,2'-BIPYRIDINE; CYTOTOXICITY; PD(II); ANION; DRUGS;
D O I
10.2174/1573406411666150504123415
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of palladium complexes with 2,2 '-bipyridine and 1-(substituted benzyl) azetidine-3, 3-dicarboxylates as ligands were synthesized and characterized by IR, 1H-NMR, ESI-MS spectra and elemental analysis. The in vitro cytotoxicity assays were carried out against A549, HCT-116, HepG-2 and SGC7901 cancer cell lines. The result showed that most of the complexes possessed moderate antiproliferative activity against HCT-116, HepG-2 and SGC7901 cell lines. Complex 12 (with 2,2 '-bipyridine and 1-(3-methoxylbenzyl) azetidine-3,3-dicarboxylate as ligand) was the most potent antitumor agent among all thirteen complexes, which showed comparable or better cytotoxicity against all four tested cancer cell lines than carboplatin. The interaction between complex 12 and pET22b plasmid DNA was investigated by agarose gel electrophoresis, and the result of the study showed that complex 12 had no obvious interaction with the plasmid DNA.
引用
收藏
页码:701 / 707
页数:7
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