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Dual inhibitors of hepatitis C virus and hepatocellular carcinoma: design, synthesis and docking studies

机译:丙型肝炎病毒和肝细胞癌的双重抑制剂:设计,合成和对接研究

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摘要

Aim: Simultaneous inhibition of hepatitis C virus (HCV) and hepatocellular carcinoma (HCC) may enhance anti-HCV effects and reduce resistance and side effects. Results/methodology: Novel hybrid derivatives were designed and synthesized to exhibit dual activity against HCV and its associated major complication, HCC. The synthesized compounds were screened for their potential activity against HCV and HCC. Compounds 5f, 5j, 5l, 5p, 5q, 5r, 6c and 6d exhibited potential in vitro anticancer activity against HCC cell line HepG2, while compounds 5a, 5l, 5p and 5v showed in vitro anti-HCV activity. Docking studies suggested that the newly synthesized compounds could suppress HCC through VEGFR2 tyrosine kinase inhibition. Conclusion: Compounds 5l and 5p exhibited dual activity against HCV and HCC in vitro.
机译:目的:同时抑制丙型肝炎病毒(HCV)和肝细胞癌(HCC)可能会增强抗HCV的作用,并降低耐药性和副作用。结果/方法:设计并合成了新型杂种衍生物,以表现出针对HCV及其相关主要并发症HCC的双重活性。筛选合成的化合物对HCV和HCC的潜在活性。化合物5f,5j,5l,5p,5q,5r,6c和6d表现出潜在的针对HCC细胞系HepG2的体外抗癌活性,而化合物5a,5l,5p和5v表现出体外抗HCV活性。对接研究表明,新合成的化合物可通过抑制VEGFR2酪氨酸激酶抑制HCC。结论:化合物5l和5p在体外对HCV和HCC具有双重活性。

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