title: Synthesis of 9-(2-beta-C-methyl-beta-d-ribofuranosyl)-6-substituted purine derivatives as inhibitors of HCV RNA replication.
abstract: A series of 9-(2'-beta-C-methyl-beta-d-ribofuranosyl)-6-substituted purine derivatives were synthesized as potential inhibitors of HCV RNA replication. Their inhibitory activities in a cell based HCV replicon assay were reported. A prodrug approach was used to further improve the potency of these compounds by increasing the intracellular levels of 5'-monophosphate metabolites. These nucleotide prodrugs showed much improved inhibitory activities of HCV RNA replication.
authors.affiliation: Valeant Pharmaceuticals International, 3300 Hyland Avenue Costa Mesa, CA 92626, USA. yding@icnpharm.com
authors.forename: Yili
authors.initials: Y
authors.lastname: Ding
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Girardet
authors.forename: Zhi
authors.initials: Z
authors.lastname: Hong
authors.forename: Vicky C H
authors.initials: VC
authors.lastname: Lai
authors.forename: Haoyun
authors.initials: H
authors.lastname: An
authors.forename: Yung-Hyo
authors.initials: YH
authors.lastname: Koh
authors.forename: Stephanie Z
authors.initials: SZ
authors.lastname: Shaw
authors.forename: Weidong
authors.initials: W
authors.lastname: Zhong
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis*; D002460:Cell Line; D016174:Hepacivirus / Q000235:genetics*; D006801:Humans; D011355:Prodrugs / Q000138:chemical synthesis / Q000494:pharmacology; D011684:Purine Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology; D012367:RNA, Viral / Q000187:drug effects / Q000235:genetics; D012093:Replicon / Q000187:drug effects; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents; D011355:Prodrugs; D011684:Purine Nucleosides; D012367:RNA, Viral