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 |
| 关键词 | Anti-HBV activity Protostane-type triterpene Alisol A Derivatives Chemical modification |
| ISSN号 | 0960-894X |
| DOI | 10.1016/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 IC50 values of 0.0048, 0.0044, and 0.014 mM, respectively, HBeAg with IC50 values of 0.011, 0.012, and 0.018 mM, respectively, and remarkable selective index values SIHBsAg > 333, SIHBeAg > 145; SIHBsAg = 209, SIHBeAg = 77; and SIHBsAg > 200, SIHBeAg > 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. |
| WOS关键词 | ALISOL-A ; CONSTITUENTS ; TRITERPENES ; TYPE-1 ; ALKALOIDS |
| 资助项目 | 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] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000271430400036 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279070]  |
| 专题 | 上海药物代谢研究中心 科研与新药推进处 |
| 通讯作者 | Chen, Ji-Jun |
| 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：上海药物研究所
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