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题名: Anti-HBV agents. Part 3: Preliminary structure-activity relationships of tetra-acylalisol A derivatives as potent hepatitis B virus inhibitors
作者: Zhang, Quan1; Jiang, Zhi-Yong1; Luo, Jie1; Ma, Yun-Bao1; Liu, Ji-Feng1; Guo, Rui-Hua1; Zhang, Xue-Mei1; Zhou, Jun1; Niu, Wei2; Du, Fei-Fei2; Li, Li2; Li, Chuan2; null(陈纪军)1
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
关键词: Anti-HBV activity ; Protostane-type triterpene ; Alisol A ; Derivatives ; Chemical modification
英文摘要: Thirty-two tetra-acylated derivatives of alisol A were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. Among the series of alisol A derivatives examined, five analogues were active against HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) secretion in HepG 2.2.15 cells. These results also provide interesting structure-activity relationships of tetra-acylalisol A derivatives. Compounds tetra-acetyl alisol A (A1), tetra-methoxyacetyl alisol A (A23), and tetra-ethoxyacetyl alisol A (A24) exhibited high activities against secretion of HBsAg with IC(50) values of 0.0048, 0.0044, and 0.014 mM, respectively, HBeAg with IC(50) values of 0.011, 0.012, and 0.018 mM, respectively, and remarkable selective index values SI(HBsAg) > 333, SI(HBeAg) > 145; SI(HBsAg) = 209, SI(HBeAg) = 77; and SI(HBsAg) > 200, SI(HBeAg) > 156, respectively. Additional studies in rats showed that compound A1 has favorable pharmacokinetic prosperities for further development purpose, with elimination half-time (t(1/2)) of 1.63 h and oral bioavailability (F) of 40.9%. (C) 2009 Elsevier Ltd. All rights reserved.
出版日期: 2009-12-01
卷号: 19, 期号:23, 页码:6659-6665
DOI标识: 10.1016/j.bmcl.2009.10.006
语种: 英语
ISSN号: 0960-894X
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内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/4138
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources W China, Kunming Inst Bot, Kunming 650204, Peoples R China
2.Chinese Acad Sci, Shanghai Ctr DMPK Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China

Recommended Citation:
Zhang, Q; Jiang, ZY; Luo, J; Ma, YB; Liu, JF; Guo, RH; Zhang, XM; Zhou, J; Niu, W; Du, FF; Li, L; Li, C; Chen, JJ.Anti-HBV agents. Part 3: Preliminary structure-activity relationships of tetra-acylalisol A derivatives as potent hepatitis B virus inhibitors,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2009,19(23):6659-6665
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