Design, synthesis and in vitro cytotoxicity of novel dinuclear platinum(II) complexes

被引：18
|
作者：
Gao, Chuanzhu [2 ,3 ]
Gou, Shaohua [1 ,2 ,3 ]
Fang, Lei [1 ,2 ,3 ]
Zhao, Jian [2 ,3 ]
机构：
[1] Southeast Univ, Jiangsu Prov Hitech Key Lab Biomed Res, Nanjing 211189, Peoples R China
[2] Southeast Univ, Sch Chem & Chem Engn, Nanjing 211189, Peoples R China
[3] Southeast Univ, Pharmaceut Res Ctr, Nanjing 211189, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 06期
基金：
中国国家自然科学基金;
关键词：
1R; 2R-Diaminocyclohexane derivative; Dinuclear platinum(II) complexes; Antitumor activity; ANTITUMOR-ACTIVITY; CELL-LINES; BINDING; INDUCTION; CISPLATIN; APOPTOSIS; TOXICITY; CANCER; SERIES;
D O I：
10.1016/j.bmcl.2011.01.064
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Five dinuclear platinum(II) complexes with a novel chiral ligand, 2-(((1R,2R)-2-aminocyclohexylamino)methyl)phenol (HL), were designed, prepared and spectrally characterized. In vitro cytotoxicity of all the resulting platinum(II) compounds was evaluated against human HEPG-2, A549 and HCT-116 cell lines, respectively. Results indicated that all compounds showed positive biological activity. Particularly, compound D4 has lower IC50 values than carboplatin toward HEPG-2 and A549, while compound D5 shows better activity than carboplatin against A549. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1763 / 1766
页数：4
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