Letters in Drug Design & Discovery

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

DOI: 10.2174/1570180811666140121234834

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

Page: [742 - 748] Pages: 7

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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.

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