Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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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 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.

Graphical Abstract:


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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Article Details

VOLUME: 11
ISSUE: 6
Page: [742 - 748]
Pages: 7
DOI: 10.2174/1570180811666140121234834