Synthesis, DNA binding, and cytotoxicity activity of bis-naphalenyl compounds with different diamine linkers

Synthesis, DNA binding, and cytotoxicity activity of bis-naphalenyl compounds with different... A series of novel bis-naphalenyl compounds with different diamine linkers were synthesized and characterized by 1H NMR, 13C NMR, and HR-MS. The DNA binding abilities of the compounds were studied by using flourescence titration, DNA thermal denaturation experiments, viscosity titration, and NMR studies. The DNA binding abilities of all the bis-naphalenyl compounds were on the same order of magnitude. Compared with the groove binding mode of the monomer, the bis-naphalenyl compounds exhibited partial intercalating binding mode. The cytotoxicity activities of the compounds were evaluated by MTT assay in vitro. According to the results of MTT assay, bis-naphalenyl compound 3c with hexamethylenediamine linker, and 3d with p-xylylenediamine linker were found to be more toxic against BGC823 cells. The IC50 values of the two compounds were similar to that of the control drug (5-Fluorouracil) on BGC823 cells. Compared with the results on BGC823 cells, better results were found on SW480 cells. Compounds 3c and 3d exhibited smaller IC50 values than that of control drug (5-Fluorouracil). The IC50 values of 3c, 3d, and 5-Fluorouracil were 52.01, 66.09, and 230.11 μM, respectively. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Synthesis, DNA binding, and cytotoxicity activity of bis-naphalenyl compounds with different diamine linkers

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Publisher
Springer Journals
Copyright
Copyright © 2016 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-016-2539-2
Publisher site
See Article on Publisher Site

Abstract

A series of novel bis-naphalenyl compounds with different diamine linkers were synthesized and characterized by 1H NMR, 13C NMR, and HR-MS. The DNA binding abilities of the compounds were studied by using flourescence titration, DNA thermal denaturation experiments, viscosity titration, and NMR studies. The DNA binding abilities of all the bis-naphalenyl compounds were on the same order of magnitude. Compared with the groove binding mode of the monomer, the bis-naphalenyl compounds exhibited partial intercalating binding mode. The cytotoxicity activities of the compounds were evaluated by MTT assay in vitro. According to the results of MTT assay, bis-naphalenyl compound 3c with hexamethylenediamine linker, and 3d with p-xylylenediamine linker were found to be more toxic against BGC823 cells. The IC50 values of the two compounds were similar to that of the control drug (5-Fluorouracil) on BGC823 cells. Compared with the results on BGC823 cells, better results were found on SW480 cells. Compounds 3c and 3d exhibited smaller IC50 values than that of control drug (5-Fluorouracil). The IC50 values of 3c, 3d, and 5-Fluorouracil were 52.01, 66.09, and 230.11 μM, respectively.

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Apr 8, 2016

References

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