摘要
合成了二乙烯三胺、三乙烯四胺和四乙烯五胺等低分子量聚乙烯胺类修饰的萘酰亚胺衍生物.通过UV-Vis谱、荧光光谱、圆二色谱和热变性试验研究了合成化合物与小牛胸腺DNA的键合行为,同时通过四甲基偶氮唑蓝(MTT)染色法研究了化合物对Bel-7402(人肝癌细胞)、HL-60(白血病细胞)、A549(人肺癌细胞)和Hela(人宫颈癌细胞)等细胞株的体外抗肿瘤活性,化合物NI1对A549细胞显示良好的抑制活性,优于阳性对照顺铂.
A series of novel low molecular weight poly（ethylene imine）（diethylenetriamine,triethylenetetraamine and tetraethylenepentamine） modified naphthalimide derivatives at 4 position as the DNA binding agents were designed and synthesized.Their DNA binding properties were investigated by UV-Vis,fluorescence and circular dischroism（CD） spectroscopies and thermal denaturation experiment.Furthermore,the anticancer activity was evaluated against different tumor cell lines（human hepatocellular carcinoma Bel-7402,cells,human promyelocytic leukemia HL-60 cells,human lung cancer A549 cell,human cervical carcinoma Hela cell）.Compound NI1 exhibited potent anticancer activity against A549 cell line with IC50 value of 3.16 μmol/L,which was better than the positive control drug（cisplatin）.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2012年第4期696-702,共7页
Chinese Journal of Organic Chemistry
基金
科技部973预研(No.2010CB534913)
国家自然科学基金(Nos.21002020,21172051)
河北省自然科学基金(No.B2011201052)
河北省教育厅基金(No.2010106)
保定市科技局基金(No.11ZF123)资助项目~~
关键词
萘酰亚胺
DNA键合
聚乙烯胺
抗肿瘤
naphthalimide
DNA binding
poly（ethylene imine）
anticancer
