Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.
Eur J Med Chem. 2013 Apr;62:158-67. doi: 10.1016/j.ejmech.2012.09.017. Epub 2012 Sep 20.
We have synthesized a series of novel isoflavone analogs and evaluated their anti-HBV and anti-cancer activities in vitro. The bioassays showed that the majority of the resultant compounds exerted inhibitory effects on HBsAg and HBeAg levels, HBV DNA replication, as well as the growth of four human cancer cell lines to various extents, which supported the rationale of the design. In particular, compound 8f showed the highest activity against HBV infection and HBV-related liver cancer. Compound 7l (IC50 = 0.47 μM) also exerted remarkable inhibitory effect on the growth lung cancer cell line A-549.
我们合成了一系列新的异黄酮类似物，并在体外评估了它们的抗乙肝病毒和抗癌活性。生物测定结果表明，大多数所得化合物对 HBsAg 和 HBeAg 水平、HBV DNA 复制以及四种人癌细胞系的生长均有不同程度的抑制作用，这支持了设计的合理性。特别是化合物 8f 对乙肝病毒感染和乙肝相关肝癌表现出最高的活性。化合物 7l（IC50=0.47 μM）对肺癌细胞系 A-549 的生长也表现出显著的抑制作用。
