Synthesis and biological evaluation of novel dinuclear platinum(II) complexes derived from a novel chiral ligand
Synthesis and biological evaluation of novel dinuclear platinum(II) complexes derived from a novel chiral ligand
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DOI：
10.1016/j.ica.2016.10.032
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发表时间：
2017-01
影响因子：
2.8
通讯作者：
Zhuxin Zhang;Chunli Li;Xiao-Jian Sun;Chuanzhu Gao;Cong Yu;L. Qinghua;Bai Linkui;Y. Qian;Bo Yang;P. Dong;Yingjie Zhang
中科院分区：
文献类型：
--
作者：
Zhuxin Zhang;Chunli Li;Xiao-Jian Sun;Chuanzhu Gao;Cong Yu;L. Qinghua;Bai Linkui;Y. Qian;Bo Yang;P. Dong;Yingjie Zhang
以（1 R，1′R，2 R，2′R）-N1，N1′-（1，2-亚苯基双（亚甲基））二环己二胺（HL）为载体，设计、合成并表征了6个新型双核铂（II）配合物。对中间体[Pt 2 I4 L]和化合物A1-A6进行了IR、1H NMR、ESI-MS和元素分析表征。琼脂糖凝胶电泳结果表明，新合成的化合物具有与顺铂相似的DNA解旋能力。此外，通过MTT法评价了这些金属配合物对HepG-2、A549、HCT-116和MCF-7细胞系的体外细胞毒性。结果表明，所有目标配合物对HEPG-2、A549和HCT-116细胞株均表现出抗肿瘤活性。化合物A2对HepG-2和A549细胞株的细胞毒活性优于卡铂，对卡铂不敏感的HCT-116细胞株也有一定的抑制作用。化合物Al对HepG-2和A549细胞系的抗癌活性与卡铂相似。
As the carrier group, six novel dinuclear platinum(II) complexes with a tetradentate ligand, (1R,1′R,2R,2′R)-N1,N1′-(1,2-phenylenebis(methylene))dicyclohexane-1,2-diamine (HL), have been designed, synthesized and characterized. To characterize the intermediate [Pt2I4L] and compounds A1–A6 IR,1H NMR and ESI-MS spectroscopies and element analysis were applied. The newly synthesized compounds possessed DNA unwinding capability similar to cisplatin by the means of agarose gel electrophoresis. In addition, the evaluation of these metal complexes in vitro cytotoxicities against HepG-2, A549, HCT-116 and MCF-7 cell lines were conducted by MTT assay. According to the results, all targeted complexes exhibited antitumor activity against HEPG-2, A549 and HCT-116 cell lines. Compound A2 showed better cytotoxicity than carboplatin against HepG-2 and A549 cell lines and also presented a certain activity against HCT-116 which are insensitive to carboplatin. The anticancer activity of Compound A1 was similar to carboplatin on HepG-2 and A549 cell lines.