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

Content Provider	Springer Nature Link
Author	Huang, Yu Song, Yu Huang, Min Fan, Yan Ru Tian, Da Nian Zhao, Qi Peng Yang, Xin Bin Zhang, Wan Nian
Copyright Year	2016
Abstract	A series of novel bis-naphalenyl compounds with different diamine linkers were synthesized and characterized by $^{1}$H NMR, $^{13}$C 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 IC$_{50}$ 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 IC$_{50}$ values than that of control drug (5-Fluorouracil). The IC$_{50}$ values of 3c, 3d, and 5-Fluorouracil were 52.01, 66.09, and 230.11 μM, respectively.
Starting Page	7329
Ending Page	7344
Page Count	16
File Format	PDF
ISSN	09226168
Journal	Research on Chemical Intermediates
Volume Number	42
Issue Number	10
e-ISSN	15685675
Language	English
Publisher	Springer Netherlands
Publisher Date	2016-04-08
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Bis-naphalenyl compounds Diamine linkers Cytotoxicity activity DNA binding Catalysis Physical Chemistry Inorganic Chemistry
Content Type	Text
Resource Type	Article
Subject	Chemistry

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