Synthesis and anti-integrase evaluation of novel calix[4]arene derivatives containing the triazolyl 1,3-diketo moiety

被引：0

作者：

Zai-Gang Luo ^{[1
]}

Yu Zhao ^{[1
]}

Chao Ma ^{[1
]}

Xue-Mei Xu ^{[1
]}

Xiao-Mei Zhang ^{[1
]}

Nian-Yu Huang ^{[2
]}

Hong-Qiu He ^{[3
]}

机构：

[1] College of Chemical Engineering,Anhui University of Science & Technology

[2] College of Chemistry and Life Sciences,China Three Gorges University

[3] Chongqing Center for Biomedicines and Medical Equipment,Chongqing Academy of Science and Technology

来源：

Chinese Chemical Letters | 2014年 / 25卷 / 05期

基金：

中国国家自然科学基金;

关键词：

HIV-1 integrase inhibitor; Calix[4]arene derivative; 2; 3-Triazole; 3-Diketo; Strand transfer;

D O I：

暂无

中图分类号：

TQ464.8 [酶及辅酶];

学科分类号：

100705 ;

摘要：

A series of novel calix[4]arene derivatives incorporating two triazolyl 1 3-diketo subunits in alternate positions at the lower rim were synthesized and screened for HⅣ integrase inhibition activity.The chemical structures of these compounds were confirmed by means of1H NMR 13C NMR,and ESI-MS.Preliminary bioassays indicated that calix[4]arene derivatives proved to be more active than p-tertbutylcalix[4]arene derivatives.In particular,compound 4g presented the most potent integrase strand transfer inhibitory activity with an IC50value of 6.1 mmol/L.

引用

页码：737 / 740

页数：4

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