Design, Synthesis, and Bioactive Screen In Vitro of Cyclohexyl (E)-4-(Hydroxyimino)-4-Phenylbutanoates and Their Ethers for Anti-Hepatitis B Virus Agents.
作者： Xinhua Cui , Min Zhou , Jie Tan , Zhuocai Wei , Wanxing Wei
DOI: 10.3390/MOLECULES24112063
关键词:
摘要: A series of oxime Cyclohexyl (E)-4-(hydroxyimino)-4-phenylbutanoates and their ethers were designed, synthesized, evaluated for anti-hepatitis B virus (HBV) activities with HepG 2.2.15 cell line in vitro. Most these compounds possessed anti-HBV activities, among them, compound 4B-2 showed significant inhibiting effects on the secretion HBsAg (IC50 = 63.85 ± 6.26 μM, SI 13.41) HBeAg 49.39 4.17 17.34) comparing to lamivudine (3TC) 234.2 17.17 2.2) 249.9 21.51 2.07). Docking study binding a protein residue (PDB ID: 3OX8) from HLA-A2 that immunodominant HBcAg18-27 epitope (HLA-A2.1- restricted CTL epitope) active site was carried out by using molecular operation environment (MOE) software. results behaviors HLA-A partly coincided vitro screening.
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