Synthesis of 9-(2-β-C-methyl-β-D-ribofuranosyl)-6-substituted purine derivatives as inhibitors of HCV RNA replication

Y Ding, JL Girardet, Z Hong, VCH Lai, H An…

Index: Ding, Yili; Girardet, Jean-Luc; Hong, Zhi; Lai, Vicky C.H.; An, Haoyun; Koh, Yung-Hyo; Shaw, Stephanie Z.; Zhong, Weidong Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 3 p. 709 - 713

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Citation Number: 32

Abstract

A series of 9-(2′-β-C-methyl-β-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 ...