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Synthesis and biological evaluation of phenylpropanoid derivatives

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Abstract

In this work, a series of oxime ether phenylpropanoid derivatives were synthesized. Their anti-hepatitis B virus (HBV) activity in HepG 2.2.15 cells was determined, and anti-cancer potential against three human cancer cell lines was evaluated. All the synthesized derivatives showed great efficiency against HBV. Compound 4d demonstrated the most effective anti-HBV activity, performing strong potent inhibitory not only on the secretion of HBsAg (IC50 = 50.45 μM, SI = 9.18) and HBeAg (IC50 = 50.11 μM, SI = 9.24), but also on the HBV DNA replication (IC50 = 51.80 μM, SI = 8.94). Besides, the synthetic compounds also displayed obvious anti-cancer activity. Moreover, the docking study of all synthesized compounds inside the related protein active site was conducted to explore the molecular interactions and a molecular target for activity using a MOE-docking technique. This study identified a new class of potent anti-HBV and anti-cancer agents.

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Acknowledgments

This work was financially supported by the national natural science foundation of China, natural science foundation of Guangxi province, China, and science research and technology development foundation of Guangxi province, China.

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Authors and Affiliations

  1. College of Science, Guangdong Ocean University, Zhanjiang, 524088, People’s Republic of China

    Sheng Liu & Yubin Li

  2. Department of Chemistry, Guangxi University, Nanning, 530004, People’s Republic of China

    Sheng Liu & Wanxing Wei

  3. Department of Pharmacology, Guilin Medical University, Guilin, 541004, People’s Republic of China

    Jingchen Wei

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  1. Sheng Liu
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  2. Yubin Li
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Correspondence to Sheng Liu or Wanxing Wei.

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Liu, S., Li, Y., Wei, W. et al. Synthesis and biological evaluation of phenylpropanoid derivatives. Med Chem Res 25, 1074–1086 (2016). https://doi.org/10.1007/s00044-016-1554-6

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