Synthesis and biological evaluation of phenylpropanoid derivatives |
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Authors: | Sheng Liu Yubin Li Wanxing Wei Jingchen Wei |
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Affiliation: | 1.College of Science,Guangdong Ocean University,Zhanjiang,People’s Republic of China;2.Department of Chemistry,Guangxi University,Nanning,People’s Republic of China;3.Department of Pharmacology,Guilin Medical University,Guilin,People’s Republic of China |
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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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