新型抗乙型肝炎病毒药物白头翁苷衍生物的合成、构效关系及生物评价。
Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents.
机构信息
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China.
出版信息
Bioorg Med Chem. 2012 May 1;20(9):2877-88. doi: 10.1016/j.bmc.2012.03.023. Epub 2012 Mar 16.
A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-O-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 2l, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC(50) values in the range of 2.82-7.48 μM. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC(50)=18.68 μM, 21.71 μM), HBeAg (IC(50)=13.16 μM, 33.73 μM), but also HBV DNA replication (IC(50)=7.48 μM, 3.63 μM). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents.
合成了一系列的娃儿藤定衍生物，并在 HepG2.2.15 细胞中评估了它们的抗乙型肝炎病毒 (HBV) 活性。大多数 3-O-取代的娃儿藤定衍生物表现出有效的抗 HBV 活性。在所测试的化合物中，有 6 个化合物（2e-2h、2l、2r）对 HBV DNA 复制具有显著的抑制活性，IC50 值在 2.82-7.48 μM 范围内。有趣的是，有两个化合物（2e、2f）不仅具有很强的抑制 HBsAg（IC50=18.68 μM、21.71 μM）和 HBeAg（IC50=13.16 μM、33.73 μM）分泌的活性，而且对 HBV DNA 复制也有很强的抑制活性（IC50=7.48 μM、3.63 μM）。讨论了娃儿藤定衍生物的构效关系（SARs），这对于探索和开发新型抗 HBV 药物的娃儿藤定衍生物具有重要意义。
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