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

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

Journal Name: Letters in Drug Design & Discovery

Volume 11 , Issue 6 , 2014

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Graphical 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.

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Article Details

Year: 2014
Published on: 27 May, 2014
Page: [742 - 748]
Pages: 7
DOI: 10.2174/1570180811666140121234834
Price: $65

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