Synthesis, DNA Binding Properties and Bioactivity of Naphthalimide Polyethylene imine Conjugates

Abstract

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 promyelocyte leukemia HL-60 cells, human lung cancer A549 cell, human cervical carcinoma Hela cell). Compound Nil exhibited potent anticancer activity against A549 cell line with IC 50 value of 3.16 μ,mol/L, which was better than the positive control drug (cisplatin). © 2012 Chinese Chemical Society & SIOC, CAS.