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

[ Vol. 11 , Issue. 2 ]


Liming Hu, Zhipeng Li, Zhanyang Wang, Gengxin Liu, Xianzhuo He, Xiaoli Wang and Chengchu Zeng   Pages 180 - 187 ( 8 )


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.


Aromatic diketones, desmosdumotin D, HIV IN inhibitory activity, integrase inhibitor, molecular docking.


College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China.

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