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

页码：1201 / 1205

页数：5

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