Anti-HBV agents. Part 1: Synthesis of alisol A derivatives: a new class of hepatitis B virus inhibitors.
Anti-HBV agents. Part 1: Synthesis of alisol A derivatives: a new class of hepatitis B virus inhibitors.
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DOI：
10.1016/j.bmcl.2008.07.012
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发表时间：
2008-08
影响因子：
2.7
通讯作者：
Quan Zhang;Zhi-Yong Jiang;Jie Luo;Pi Cheng;Yun-bao Ma;Xue-mei Zhang;Feng-xue Zhang;Jun Zhou;Ji-Jun Chen
中科院分区：
文献类型：
--
作者：
Quan Zhang;Zhi-Yong Jiang;Jie Luo;Pi Cheng;Yun-bao Ma;Xue-mei Zhang;Feng-xue Zhang;Jun Zhou;Ji-Jun Chen
合成了一系列茜草醇A衍生物，并对其体外抗乙型肝炎病毒（HBV）活性和细胞毒性进行了评价。初步研究表明，对艾里索A的亲本结构进行简单的修饰可以产生许多潜在的重要的抗HBV衍生物。其中抗HBV活性最高的化合物6a对HBV表面抗原（IC50=0.024mM）、HBV e抗原（IC50=0.028mM）的分泌具有较高的抑制活性，对SIHBsAg >08、SIHBeAg bbb93的选择性指标也有显著的抑制作用，可作为一种新型的HBV抑制剂进行进一步评价。
A series of alisol A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. The preliminary investigation demonstrates that simple modifications of the parent structure of alisol A can produce a number of potentially important derivatives against HBV. The most active anti-HBV compound 6a showed high activities against the secretion of HBV surface antigen (IC50=0.024mM), HBV e antigen (IC50=0.028mM) and remarkable selective indices (SIHBsAg>108, SIHBeAg>93), which was selected for further evaluation as a novel HBV inhibitor.