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

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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), C23H18N4, was structurally determined by single-crystal X-ray diffraction. It crystallizes in the triclinic system, space group P with a = 9.585(4), b = 9.684(4), c = 11.339(5) Å, β = 88.250(7)º, V = 925.3(6), Z = 2, Dc = 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.

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	霍丽妮
	陈睿
	廖艳芳
	刘华钢
	李培源
	卢汝梅
	钟振国

关键词 ： acridine-1,2,3-triazole, crystal structure, antitumor activities

Abstract：

Key words： acridine-1,2,3-triazole crystal structure antitumor activities

收稿日期: 2015-12-28 出版日期: 2016-05-12

基金资助: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), and the Scientific Research Fund of Guangxi University of Chinese Medicine (No. QN14017, 2015MS003)

通讯作者: 58251323@163.com E-mail: 58251323@163.com

引用本文:

霍丽妮;陈睿;廖艳芳;刘华钢;李培源;卢汝梅;钟振国. Synthesis, Crystal Structure and Biological Evaluation of Acridine-1,2,3-triazole Derivatives[J]. 结构化学, 2016, 35(5): 698-704.
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. CHINESE JOURNAL OF STRUCTURAL CHEMISTRY, 2016, 35(5): 698-704.

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http://manu30.magtech.com.cn/jghx/CN/ 或 http://manu30.magtech.com.cn/jghx/CN/Y2016/V35/I5/698

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