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

[ Vol. 11 , Issue. 2 ]

Author(s):

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

Abstract:


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.

Keywords:

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

Affiliation:

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

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