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

详细信息    查看全文

• 作者：Yu Huang ; Yu Song ; Min Huang ; Yan-Ru Fan…
• 关键词：Bis ; naphalenyl compounds ; Diamine linkers ; Cytotoxicity activity ; DNA binding
• 刊名：Research on Chemical Intermediates
• 出版年：2016
• 出版时间：October 2016
• 年：2016
• 卷：42
• 期：10
• 页码：7329-7344
• 全文大小：1,276 KB
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Catalysis
  Physical Chemistry
  Inorganic Chemistry
  
• 出版者：Springer Netherlands
• ISSN：1568-5675
• 卷排序：42

文摘

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.