Study on the cytotoxic activity of platinum(II) complexes of (1R,2R)-N1-cyclopentyl-1,2-cyclohexanediamine with substituted malonate derivatives

被引：11
|
作者：
Zhou, Zhiping [1 ,2 ]
Chen, Feihong [1 ,2 ,3 ]
Xu, Gang [1 ,2 ,3 ]
Gou, Shaohua [1 ,2 ,3 ]
机构：
[1] Southeast Univ, Pharmaceut Res Ctr, Nanjing 211189, Jiangsu, Peoples R China
[2] Southeast Univ, Sch Chem & Chem Engn, Nanjing 211189, Jiangsu, Peoples R China
[3] Southeast Univ, Jiangsu Prov Hitech Key Lab Biomed Res, Nanjing 211189, Jiangsu, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 02期
基金：
中国国家自然科学基金;
关键词：
Platinum(II) complexes; Cyclopentyl; Malonate derivatives; Cytotoxicity; Anticancer; N-MONOALKYL; 1R; 2R-DIAMINOCYCLOHEXANE; IN-VITRO; CARRIER LIGANDS; PHASE-II; CANCER; PICOPLATIN; CARBOPLATIN; CISPLATIN; THERAPY; DESIGN;
D O I：
10.1016/j.bmcl.2015.12.019
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Three platinum(II) complexes of (1R,2R)-N-1-cyclopentyl-1,2-cyclohexanediamine with malonate derivatives were designed, synthesized and spectrally characterized. MTT assay showed that the complexes possessed positive cytotoxic effect on the four human solid tumor cell lines. Among the complexes, complex 2 demonstrated the strongest cytotoxic activity compared to cisplatin and oxaliplatin against HepG2 cell line (IC50 = 3.04 mu M). Furthermore, the results of gel electrophoresis revealed that complex 2 interacted with DNA in a different mode from that of cisplatin. Mechanism studies of cell proliferation inhibition and cellular uptake indicated that complex 2 entered HepG2 cell more efficiently than cisplatin, exhibited massive G2 accumulation and then induced apoptosis. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码：322 / 327
页数：6
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