Synthesis, Crystal Structures, and Binding Behaviors with CT-DNA/BSA, Antimicrobial and Cytotoxic Activities of Three New Pyrazine Acylhydrazones  

作　　者：YANG Jie LIU Xiang-Rong LIAO Geng-Hui YU Ming-Kun YANG Zai-Wen ZHAO Shun-Sheng 杨杰;刘向荣;廖庚晖;于明坤;杨再文;赵顺省(College of Chemistry and Chemical Engineering,Xi’an University of Science and Technology,Xi’an 710054,China)

机构地区：[1]College of Chemistry and Chemical Engineering,Xi’an University of Science and Technology,Xi’an 710054,China

出　　处：《Chinese Journal of Structural Chemistry》2020年第9期1639-1654,1555,共17页结构化学（英文）

基　　金：supported by the National Natural Science Foundation of China(Nos.U1903033,21073139 and 21373158);Science and Technology on Combustion and Explosion Laboratory Foundation of Shaanxi(No.6142603010301)。

摘　　要：Three new acylhydrazones containing pyrazine ring(C12H11N5O2·CH3COOH,1;C13H13N5O·2CH3COOH,2;C13H13N5O3·C13H13N5O3,3)were synthesized and fully characterized.The single-crystal XRD indicated that both 1 and 2 crystallized in monoclinic,P21/c space group but 3 belonged to monoclinic,C2/c space group.The temperature of the maximum thermal decomposition peaks measured by thermogravimetry for 1~3 is 284,289 and 276℃respectively,all showing better thermal stabilities.The interactions of 1~3 with calf thymus DNA(CT-DNA)and bovine serum albumin(BSA)were studied by UV-Vis absorption spectroscopy and fluorescence spectroscopy,respectively,presenting that 1~3 could bind to CT-DNA via groove binding mode and quench the fluorescence of BSA through static process.Moreover,molecular docking studies of the interactions between 1~3 with DNA/BSA were in good agreement with experimental results.From antimicrobial activities of 1~3 and gentamycin sulfate against Staphylococcus aureus,Escherichia coli and Salmonella typhimurium,it was inferred that 3 had generally stronger antibacterial activity than 1 and 2 and is more active against Staphylococcus aureus than gentamycin sulfate.The cytotoxic tests of 1~3 and etoposide on human lung cancer cells(A549)were carried out by using the MTT method.

关 键 词：ACYLHYDRAZONE crystal structure CT-DNA/BSA binding antimicrobial activity cytotoxic activity 

分 类 号：TQ460.1[化学工程—制药化工]