Citation: HUO Li-Ni, CHEN Rui, LIAO Yan-Fang, LIU Hua-Gang, LI Pei-Yuan, LU Ru-Mei, ZHONG Zhen-Guo. Synthesis, Crystal Structure and Biological Evaluation of Acridine-1,2,3-triazole Derivatives[J]. Chinese Journal of Structural Chemistry, ;2016, 35(5): 698-704. doi: 10.14102/j.cnki.0254-5861.2011-1100 shu

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

a.
a. College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530001, China;
b.
b. Faculty of Chinese Medicine Science, Guangxi University of Chinese Medicine, Nanning 530222, China;
c.
c. Guangxi Research Institute of Chemical Industry, Nanning 530001, China;
d.
d. Guangxi Medical University, Nanning 530021, China

Corresponding author: CHEN Rui,
Received Date: 28 December 2015
Available Online: 18 March 2016
Fund Project: Supported by the National Natural Science Foundation of China (No. 51263002) (No. 51263002) Natural Science Foundation of Guangxi Province (No. 2014GXNSFBA118182) (No. 2014GXNSFBA118182) the Scientific Research Fund of Guangxi Provincial Education Department (No. YB2014181) (No. YB2014181) Ministry of Education of China (CMEMR2015-B04) (Guangxi Normal University) and the Scientific Research Fund of Guangxi University of Chinese Medicine (No. QN14017, 2015MS003) (CMEMR2015-B04)

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), C₂₃H₁₈N₄, 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) Å, β = 88.250(7)°, V = 925.3(6), Z = 2, D_c= 1.258 g/cm³, 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.
- acridine-1,2,
- 3-triazole,
- crystal structure,
- antitumor activities
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