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Anti-HBV agents. Part 3: Preliminary structure-activity relationships of tetra-acylalisol A derivatives as potent hepatitis B virus inhibitors

文献类型：期刊论文

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
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2009-12-01
卷号19期号:23页码:6659-6665
ISSN号0960-894X
关键词Anti-hbv Activity Protostane-type Triterpene Alisol a Derivatives Chemical Modification
DOI10.1016/j.bmcl.2009.10.006
文献子类Article
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.
学科主题Chemistry, Medicinal ; Chemistry, Organic
WOS关键词ALISOL-A ; CONSTITUENTS ; TRITERPENES ; TYPE-1 ; ALKALOIDS
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000271430400036
资助机构National Natural Science Foundation of China (NSFC) [30672522]; New Drug Development, Ministry of Science and Technology [2009ZX09103- 108]; Chinese Academy of Sciences [GJHZ200818]; CAS- Croucher Foundation [CAS- CF07/08. SC03]
公开日期2012-03-21
源URL[http://ir.kib.ac.cn:8080/handle/151853/4138]  
专题昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室
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
推荐引用方式
GB/T 7714		 Zhang, Quan,Jiang, Zhi-Yong,Luo, Jie,et al. Anti-HBV agents. Part 3: Preliminary structure-activity relationships of tetra-acylalisol A derivatives as potent hepatitis B virus inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2009,19(23):6659-6665.
APA Zhang, Quan.,Jiang, Zhi-Yong.,Luo, Jie.,Ma, Yun-Bao.,Liu, Ji-Feng.,...&Chen, Ji-Jun.(2009).Anti-HBV agents. Part 3: Preliminary structure-activity relationships of tetra-acylalisol A derivatives as potent hepatitis B virus inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,19(23),6659-6665.
MLA Zhang, Quan,et al."Anti-HBV agents. Part 3: Preliminary structure-activity relationships of tetra-acylalisol A derivatives as potent hepatitis B virus inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 19.23(2009):6659-6665.

入库方式： OAI收割

来源：昆明植物研究所

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