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论文 |
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论文题目: |
Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents
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论文题目英文: |
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作者: |
Wang, Li-Jun; Geng, Chang-An; Ma, Yun-Bao; Huang, Xiao-Yan; Luo, Jie; Chen, Hao; Guo, Rui-Hua; Zhang, Xue-Mei; Chen, Ji-Jun
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论文出处: |
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年: |
2012
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卷: |
20 |
期: |
9 |
页: |
2877-2888 |
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发表期刊: |
BIOORGANIC & MEDICINAL CHEMISTRY |
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影响因子: |
3.075
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摘要: |
A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-O-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 2l, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC50 values in the range of 2.82-7.48 mu M. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC50 = 18.68 mu M, 21.71 mu M), HBeAg (IC50 = 13.16 mu M, 33.73 mu M), but also HBV DNA replication (IC50 = 7.48 mu M, 3.63 mu M). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents. (C) 2012 Elsevier Ltd. All rights reserved. |
英文摘要: |
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