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

HUO Li-Ni; CHEN Rui; LIAO Yan-Fang; LIU Hua-Gang; LI Pei-Yuan; LU Ru-Mei; ZHONG Zhen-Guo

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

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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) ?, 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.

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《结构化学》 |2016年第5期|698-704|共7页
作者
HUO Li-Ni; CHEN Rui; LIAO Yan-Fang; LIU Hua-Gang; LI Pei-Yuan; LU Ru-Mei; ZHONG Zhen-Guo;
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College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530001, China;

Guangxi Medical University, Nanning 530021, China;

Faculty of Chinese Medicine Science, Guangxi University of Chinese Medicine, Nanning 530222, China;

Guangxi Research Institute of Chemical Industry, Nanning 530001, China;

Guangxi Medical University, Nanning 530021, China;

College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530001, China;

College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530001, China;

College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530001, China;

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

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