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学科主题: 有机化学
题名: Discovery of Novel Arylethynyltriazole Ribonucleosides with Selective and Effective Antiviral and Antiproliferative Activity
其他题名: 具有抗增殖和抗病毒选择和有效活性的Arylethynyltriazole Ribonucleosides的发现
作者: WAN JINQIAO ; Xia Y(夏熠) ; LIU YANG ; WANG MENGHUA ; ROCCHI PALMA ; Yao JH(姚建华) ; Qu FQ(曲凡琪) ; NEYTS JOHAN ; IOVANNA JUAN L ; Peng L(彭玲)
通讯作者: 彭玲
刊名: J. Med. Chem.
发表日期: 2009
卷: 52, 期:4, 页:1144-1155
收录类别: SCI
部门归属: 武汉大学; Univ Aix Marseille 2; 上海有机所; Rega Inst
英文摘要: Novel ethynyltriazole ribonucleosides were synthesized using a simple and efficient two-step procedure involving Sonogashira coupling and subsequent ammonolysis. Compounds 2f and 3o inhibited hepatitis C virus (HCV) replication efficiently, whereas compound 3f demonstrated potent apoptosis-induced antiproliferative activity against pancreatic cancer MiaPaCa-2 cells both in vitro and in vivo. Most interestingly, the notable selective antiviral and antiproliferative activities were achieved respectively for 2f and 3f by modulating the ribose sugar moiety into deprotected and protected forms while retaining a similar trifluoromethylphenylethynyltriazole as the nucleobase. Preliminary structure-activity relationship study revealed that not only the ribose moiety but also the CF3 group at the p-position of the phenyl ring and the rigid triple bond functionality contributed critically to the observed antiviral activity of 2f against HCV and antiproliferative activity of 3f against pancreatic cancer. These two compounds constitute therefore promising leads in the search for new antiviral and anticancer candidates.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000263530200024
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/23736
Appears in Collections:计算机化学与化学信息学研究室_期刊论文

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Recommended Citation:
WAN JINQIAO,Xia Y,LIU YANG,et al. Discovery of Novel Arylethynyltriazole Ribonucleosides with Selective and Effective Antiviral and Antiproliferative Activity[J]. J. Med. Chem.,2009,52(4):1144-1155.
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