Anticancer Activity and DNA Binding of 4-Alkylenediamines Modified Naphthalimide Derivatives
Ke-Rang Wang, Feng Qian, Zi-Bo Yang, Hong-Wei An, Dan Han, Hua Chen, Ping-Zhu Zhang and Xiao-Liu Li
Affiliation: Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002, China.
Keywords: Naphthalimide, DNA intercalator, Alkylenediamines, Anticancer, DNA binding, Fluorescence.
Four naphthalimide derivatives 2-5 modified with various alkylenediamines at 4-position have been designed
and synthesized. Their anticancer activities were preliminarily evaluated, which showed potent anticancer activities
against A549 cell line with IC50 values lower than 5 µM. Furthermore, the DNA binding properties of 2 with calf thymus
(Ct) DNA were investigated by UV-Vis, fluorescence, and circular dichroism (CD) spectroscopies and thermal denaturation
experiment. The results showed that compound 2 as the DNA intercalator exhibited strong binding affinity with Ct-
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