Coumarins hinged directly on benzimidazoles and their ribofuranosides to inhibit hepatitis C virus

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題名:	Coumarins hinged directly on benzimidazoles and their ribofuranosides to inhibit hepatitis C virus
作者:	謝發坤;Tsay, Shwu-Chen;Hwu, Jih Ru;Singha, Raghunath;Huang, Wen-Chieh;Chang, Yung Hsiung;Hsu, Ming-Hua;Shieh, Fa-kuen;Lin, Chun-Cheng;Hwang, Kuo Chu;Horng, Jia-Cherng;De Clercq, Erik;Vliegen, Inge;Neyts, Johan
貢獻者:	理學院化學學系
關鍵詞:	Anti-HCV;Antiviral Agents - chemical synthesis;Antiviral Agents - chemistry;Antiviral Agents - pharmacology;Benzimidazole;Benzimidazoles - chemistry;Cell Line, Tumor;Coumarin;Coumarins - chemical synthesis;Coumarins - chemistry;Coumarins - pharmacology;Dose-Response Relationship, Drug;Furans - chemistry;Glycosides - chemical synthesis;Glycosides - chemistry;Glycosides - pharmacology;Hepacivirus - drug effects;Hinged hybride;Humans;Mass Spectrometry;Models, Chemical;Molecular Structure;Pentoses - chemistry;Ribofuranoside;Spectroscopy, Fourier Transform Infrared;Structure-Activity Relationship;Virus Replication - drug effects
日期:	2013-03-18
上傳時間:	2026-04-21 14:07:43 (UTC+8)
出版者:	Elsevier Masson SAS;France: Elsevier Masson SAS
摘要:	摘要： A new compound library that contained 20 hinged benzimidazole–coumarin hybrids and their β-d-ribofuranosides was established. The anti-hepatitis C virus (HCV) activity of all novel coumarin derivatives, which were obtained by use of organic synthetic methods, was tested. Two of these hybrids exhibited appealing EC50 values of as low as 3.0 and 5.5 μM. The best selectivity index was 14. The incorporation of a d-ribofuranose into the hinged hybrids provided the corresponding nucleosides with the β configuration, one of which inhibited HCV replication with an EC50 value of 20 μM. Additionally, the structure–activity relationship is elucidated on the basis of the functional groups that were attached to the nuclei of benzimidazole, coumarin, and ribofuranose of the hybrids. [Display omitted] A compound library containing 20 new hybrids was established by chemical synthesis. Three hybrids inhibited HCV replication with EC50 values as low as 3.0, 5.5, and 20 μM. ► A new compound library containing 20 hinged benzimidazole–coumarin hybrids was established. ► These compounds inhibited HCV replication with EC50 values as low as 3.0 μM. ► A structure–activity relationship with five guidelines is illustrated. 其他題名： Eur J Med Chem 出版者： France: Elsevier Masson SAS 出版日期： 2013-05-01 出處： European journal of medicinal chemistry, 2013-05, Vol.63, p.290-298 版權： 2013 Elsevier Masson SAS 版權： Copyright © 2013 Elsevier Masson SAS. All rights reserved. 識別號： ISSN: 0223-5234 識別號： ISSN: 1768-3254 識別號： EISSN: 1768-3254 識別號： DOI: 10.1016/j.ejmech.2013.02.008 識別號： PMID: 23501114
顯示於類別:	[化學學系] 期刊論文

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