以1-（取代苄基）氮杂环丁烷-3,3-二羧酸酯为离去基团的钯（II）配合物的设计、合成及生物学评价
Design, Synthesis and Biological Evaluation of Palladium (II) Complexes with 1-(substituted benzyl) azetidine-3,3-dicarboxylates as Leaving Group.
作者信息
Xu Gang, Lu Hua, Zhitao Jiang, Zhang Shuying, Gou Shaohua
机构信息
School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China.
出版信息
Med Chem. 2015;11(7):701-7. doi: 10.2174/1573406411666150504123415.
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, (1)H-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.
合成了一系列以2,2'-联吡啶和1-(取代苄基)氮杂环丁烷-3,3-二羧酸酯为配体的钯配合物，并通过红外光谱、(1)H-核磁共振、电喷雾电离质谱和元素分析对其进行了表征。针对A549、HCT-116、HepG-2和SGC7901癌细胞系进行了体外细胞毒性试验。结果表明，大多数配合物对HCT-116、HepG-2和SGC7901细胞系具有中等程度的抗增殖活性。配合物12（以2,2'-联吡啶和1-(3-甲氧基苄基)氮杂环丁烷-3,3-二羧酸酯为配体）是所有13种配合物中最有效的抗肿瘤剂，其对所有四种测试癌细胞系的细胞毒性与卡铂相当或更好。通过琼脂糖凝胶电泳研究了配合物12与pET22b质粒DNA之间的相互作用，研究结果表明配合物12与质粒DNA没有明显的相互作用。
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