Synthesis and in vitro activity of 4' and 5'-modified analogues of apiosyl nucleosides as potent anti-HCV agents.

Hua Li, Wonjae Lee, Joon Hee Hong

Index: Nucleosides Nucleotides Nucleic Acids 28(11) , 1104-16, (2009)

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Abstract

Novel doubly branched apio dideoxynucleosides were synthesized starting from 1,3-dihydroxyacetone using an ozonolysis and Grignard addition as key steps, and evaluated for anti-hepatitis C virus (HCV) activity. The adenine derivative 24 showed significant anti-HCV activity, indicating that the branches at the 4',5'-position of the apiosyl ring led to favorable interaction with HCV polymerase.