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.
Letters in Drug Design & Discovery
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.
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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
DOI https://dx.doi.org/10.2174/1570180811666140121234834 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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