Design, Synthesis and Biological Activity of Aromatic Diketone Derivatives as HIV-1 Integrase Inhibitors

被引：4

作者：

Hu, Liming ^{[1
]}

Li, Zhipeng ^{[1
]}

Wang, Zhanyang ^{[1
]}

Liu, Gengxin ^{[2
]}

He, Xianzhuo ^{[1
]}

Wang, Xiaoli ^{[1
]}

Zeng, Chengchu ^{[1
]}

机构：

[1] Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China

[2] Langfang Hlth Vocat Coll, Langfang 065000, Hebei, Peoples R China

来源：

MEDICINAL CHEMISTRY | 2015年 / 11卷 / 02期

基金：

美国国家科学基金会;

关键词：

Aromatic diketones; desmosdumotin D; HIV IN inhibitory activity; integrase inhibitor; molecular docking; AUTOMATED DOCKING; AIDS; MECHANISMS; CHALCONE; AGENTS;

D O I：

10.2174/1573406410666140829154131

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

A series of aromatic diketone derivatives were designed and synthesized as potential HIV-1 integrase (IN) inhibitors and evaluated to determine their ability to inhibit the strand transfer process of HIV-1 integrase. The results indicate that (Z)-1-(3-acetyl-2-hydroxy-4,6-dimethoxyphenyl)-3-hydroxy-3-(substituted) phenylprop-2-en-1-one (5a-5d) can moderately inhibit HIV-1 integrase. The cyclization and condensation products (6a-6c and 7e-7f) of compounds 5a-5d show poor inhibitory activity against HIV-1 integrase. The molecular docking results indicate that the different types of compounds act on HIV-1 integrase in different ways, and these results can explain the differences in the inhibitory activities.

引用

页码：180 / 187

页数：8

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