Conjugation of cyclodextrin with fullerene as a new class of HCV entry inhibitors

• Published in: Bioorganic & medicinal chemistry Vol. 20; no. 18; pp. 5616 - 5622
• Main Authors: Xiao, Su-long, Wang, Qi, Yu, Fei, Peng, Yi-yun, Yang, Ming, Sollogoub, Matthieu, Sinaÿ, Pierre, Zhang, Yong-min, Zhang, Li-he, Zhou, De-min
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 15-09-2012; Elsevier
• Subjects: alpha-cyclodextrin; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiviral agents; Antiviral Agents - chemical synthesis; Antiviral Agents - chemistry; Antiviral Agents - pharmacology; Biological and medical sciences; Cell Line, Tumor; Conjugate; Cyclodextrins - chemical synthesis; Cyclodextrins - chemistry; Cyclodextrins - pharmacology; Dose-Response Relationship, Drug; Fullerene; Fullerenes - chemistry; HCV entry; Hepacivirus - drug effects; Humans; Indexing in process; inhibitory concentration 50; Medical sciences; Microbial Sensitivity Tests; Molecular Structure; Pharmacology. Drug treatments; Solubility; Structure-Activity Relationship; water solubility; α-Cyclodextrin; α-Cyclodextrin; Fullerene; Conjugate; HCV entry; Virus; Cyclodextrin; Entry inhibitor; Fullerenes; Antiviral; Flaviviridae; Conjugated compound; Inclusion compound; Hepatitis C virus; Hepacivirus
• ISSN: 0968-0896; 1464-3391
• DOI: 10.1016/j.bmc.2012.07.029

An α-cyclodextrin–[60]fullerene conjugate with a flexible linker at the secondary face of α-cyclodextrin has been prepared, which displays significant water solubility and, more importantly, acts as a new class of HCV entry inhibitor with IC50 at 0.17μM level.