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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
Epub Full Text Article
DOI: 10.2174/1570180811666140121234834      Price:  $95









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

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Author(s): Ke-Rang Wang, Feng Qian, Zi-Bo Yang, Hong-Wei An, Dan Han, Hua Chen, Ping-Zhu Zhang and Xiao-Liu Li
Abstract:
Four naphthalimide derivatives 2-5 modified with various alkylenediamines at 4-position have been designed and synthesized. Their antitumor activities were preliminarily evaluated, which showed potent antitumor 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, Antitumor, DNA binding, Fluorescence
Affiliation:
Key Laboratory of Chemical Biology of Hebei Province College of Chemistry and Environmental Science Hebei University Baoding 071002 China.