Synthesis and anti-hepatitis B virus activities of Matijing-Su derivatives

被引：94

作者：

Xu, Bixue ^{[1
,2
]}

Huang, Zhengming ^{[3
]}

Liu, Changxiao ^{[4
]}

Cai, Zegui ^{[1
,2
]}

Pan, Weidong ^{[1
,2
]}

Cao, Peixue ^{[1
,2
]}

Hao, Xiaojiang ^{[1
,2
]}

Liang, Guangyi ^{[1
,2
]}

机构：

[1] Key Lab Chem Nat Prod Guizhou Prov, Guiyang 550002, Peoples R China

[2] Chinese Acad Sci, Guiyang 550002, Peoples R China

[3] 302 Hosp PLA, Beijing 100039, Peoples R China

[4] Tianjin Inst Pharmaceut Res, Tianjin 300193, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 08期

关键词：

Anti-hepatitis B virus activity; Derivatives of Matijing-Su; Synthesis; ADEFOVIR DIPIVOXIL; X-PROTEIN; LAMIVUDINE; THERAPY;

D O I：

10.1016/j.bmc.2009.03.003

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of derivatives of Matijing-Su (MTS, N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol) was synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The IC50 of compounds 9c (1.40 mu M), 9g (2.33 mu M) and 9n (2.36 mu M), etc. and the selective index of 9n (45.93) of the inhibition on the replication of HBV DNA were higher than those of the positive control lamivudine [41.59, (IC50: 82.42 mu M)]. Compounds 11d, 12a and 12e also exhibited significant anti-HBV activities. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3118 / 3125

页数：8

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