Synthesis, Crystal Structure and Biological Evaluation of Acridine-1,2,3-triazole Derivatives  

作　　者：霍丽妮 陈睿 廖艳芳 刘华钢 李培源 卢汝梅 钟振国 

机构地区：[1]College of Pharmacy, Guangxi University of Chinese Medicine [2]Guangxi Medical University [3]Faculty of Chinese Medicine Science, Guangxi University of Chinese Medicine [4]Guangxi Research Institute of Chemical Industry

出　　处：《Chinese Journal of Structural Chemistry》2016年第5期698-704,共7页结构化学（英文）

基　　金：Supported by the National Natural Science Foundation of China(No.51263002);Natural Science Foundation of Guangxi Province(No.2014GXNSFBA118182);the Scientific Research Fund of Guangxi Provincial Education Department(No.YB2014181);the Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources(Guangxi Normal University);Ministry of Education of China(CMEMR2015-B04);the Scientific Research Fund of Guangxi University of Chinese Medicine(No.QN14017,2015MS003)

摘　　要：A series of acridine-1,2,3-triazole derivatives were designed, synthesized and characterized by NMR. 1-（2-methylacridinyl）-4-（4-methyl phenyl）-1,2,3-triazole（4f）, C_（23）H_（18）N_4, was structurally determined by single-crystal X-ray diffraction. It crystallizes in the triclinic system, space group P1 with a = 9.585（4）, b = 9.684（4）, c = 11.339（5） A, β = 88.250（7）o, V = 925.3（6）, Z = 2, D_c = 1.258 g/cm^3, F（000） = 368, μ = 0.077 mm^（-1）, the final R = 0.0808 and wR = 0.2218 for 3386 observed reflections（I 〉 2σ（I））. X-ray analysis indicates that the acridine ring is almost vertical to triazole ring with the dihedral angle nearly to be 75°. The crystal packing of the compound is stabilized mainly by π-π interaction. The preliminary biological tests display that some of the title compounds possess a good anti-tumour activity against MGC-803 and T24.A series of acridine-1,2,3-triazole derivatives were designed, synthesized and characterized by NMR. 1-（2-methylacridinyl）-4-（4-methyl phenyl）-1,2,3-triazole（4f）, C_（23）H_（18）N_4, was structurally determined by single-crystal X-ray diffraction. It crystallizes in the triclinic system, space group P1 with a = 9.585（4）, b = 9.684（4）, c = 11.339（5） A, β = 88.250（7）o, V = 925.3（6）, Z = 2, D_c = 1.258 g/cm^3, F（000） = 368, μ = 0.077 mm^（-1）, the final R = 0.0808 and wR = 0.2218 for 3386 observed reflections（I 〉 2σ（I））. X-ray analysis indicates that the acridine ring is almost vertical to triazole ring with the dihedral angle nearly to be 75°. The crystal packing of the compound is stabilized mainly by π-π interaction. The preliminary biological tests display that some of the title compounds possess a good anti-tumour activity against MGC-803 and T24.

关 键 词：acridine-1 2 3-triazole crystal structure antitumor activities 

分 类 号：O626.26[理学—有机化学]