Synthesis of hemslecin A derivatives: A new class of hepatitis B virus inhibitors

被引：17
|
作者：
Guo, Rui-Hua [1 ]
Geng, Chang-An [1 ]
Huang, Xiao-Yan [1 ]
Ma, Yun-Bao [1 ]
Zhang, Quan [1 ]
Wang, Li-Jun [1 ]
Zhang, Xue-Mei [1 ]
Zhang, Rong-Ping [2 ]
Chen, Ji-Jun [1 ]
机构：
[1] Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
[2] Kunming Med Univ, Kunming 650500, Yunnan, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 05期
基金：
中国国家自然科学基金;
关键词：
Hemslecin A; Derivatives; Hepatitis B virus; SCHISANDRA-WILSONIANA; FRUITS; ALISOL;
D O I：
10.1016/j.bmcl.2013.01.024
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of hemslecin A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities, namely, inhibiting the secretion of hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and HBV DNA replication on HepG 2.2.15 cells. Most of the derivatives showed enhanced anti-HBV activities, of which compounds A1-A7, B5, C and E exhibited significant activities inhibiting HBV DNA replication with IC50 values of 2.8-11.6 mu M, comparable to that of the positive control, tenofovir. Compounds A1-A3, A5, B5, and C displayed low cytotoxicities, which resulted in high SI values of 89.7, 55.6, 77.8, >83.4, >55.8, and >150.5, respectively. Crown Copyright (C) 2013 Published by Elsevier Ltd. All rights reserved.
引用
收藏
页码：1201 / 1205
页数：5
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