Anticancer Activity and DNA Binding of 4-Alkylenediamines Modified Naphthalimide Derivatives

Title:Anticancer Activity and DNA Binding of 4-Alkylenediamines Modified Naphthalimide Derivatives

Volume: 11 Issue: 6

Author(s): Ke-Rang Wang, Feng Qian, Zi-Bo Yang, Hong-Wei An, Dan Han, Hua Chen, Ping-Zhu Zhang and Xiao-Liu Li

Affiliation:

Keywords: Naphthalimide, DNA intercalator, Alkylenediamines, Anticancer, DNA binding, Fluorescence.

Abstract: 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- DNA.

Cite this article as:

Wang Ke-Rang, Qian Feng, Yang Zi-Bo, An Hong-Wei, Han Dan, Chen Hua, Zhang Ping-Zhu and Li Xiao-Liu, Anticancer Activity and DNA Binding of 4-Alkylenediamines Modified Naphthalimide Derivatives, Letters in Drug Design & Discovery 2014; 11 (6) . https://dx.doi.org/10.2174/1570180811666140121234834