Title of article
Cyclic monophosphate prodrugs of base-modified 2′-C-methyl ribonucleosides as potent inhibitors of hepatitis C virus RNA replication
Author/Authors
Esmir Gunic، نويسنده , , Jean-Luc Girardet، نويسنده , , Kanda Ramasamy، نويسنده , , Vesna Stoisavljevic-Petkov، نويسنده , , Suetying Chow، نويسنده , , Li-Tain Yeh، نويسنده , , Robert K. Hamatake، نويسنده , , Anneke Raney، نويسنده , , Zhi Hong، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
2452
To page
2455
Abstract
A new series of heterobase-modified 2′-C-methyl ribonucleosides was synthesized and tested as inhibitors of hepatitis C virus (HCV) RNA replication. The nucleosides showed a weak inhibitory activity in a HCV replicon system (EC50 = 92 μM) and did not exhibit any cytotoxicity (CC50 > 300 μM). Cyclic monophosphate (cMP) prodrugs of the same nucleosides were synthesized and also tested in the HCV replicon system. Prodrugs exhibited strong potency (EC50 = 0.008 μM) without significant cytotoxicity (CC50 > 50 μM).
Keywords
antiviral , HCV , phosphorylation , CMP , prodrug , nucleoside
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798060
Link To Document