Synthesis and biological evaluation of novel pentacyclic triterpene α-cyclodextrin conjugates as HCV entry inhibitors
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- 作者：Sulong Xiaoa ; slxiao@bjmu.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Qi Wanga ; c ; Longlong Sia ; Xiaoshu Zhoua ; Yongmin Zhangb ; Lihe Zhanga ; Demin Zhoua ; deminzhou@bjmu.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：α-Cyclodextrin ; HCV entry inhibitor ; Pentacyclic triterpene ; Click chemistry
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：29 November 2016
- 年：2016
- 卷：124
- 期：Complete
- 页码：1-9
- 全文大小：1513 K
文摘
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A series of α-cyclodextrin-pentacyclic triterpene conjugates were synthesized and evaluated for anti-HCV entry activities.
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Compounds 15 and 18 displayed the highest anti-HCV entry activities with an IC50 of 1.18 μM and 0.25 μM, respectively.
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Compounds 15 and 18 exert their inhibitory activity at post-binding step and subsequently prevent virus entry.