Synthesis and Biological Activity of 5′,9-Anhydro-3-Purine-ISONucleosides as Potential Anti-Hepatitis C Virus Agents

Abstract

In order to study structure-activity relationships among the derivatives and congeners of 5′,9-anhydro-3-(β-D-ribofuranosyl)xanthine for anti-hepatitis C virus activity, a series of 5′,9-anhydro-purine-isonucleosides with a substituent (s) at 6- or/and 8-position of the purine moiety were synthesized, and their anti-hepatitis C virus activity and cytotoxicity were evaluated and discussed.

Keywords:

• 5′,9-Anhydro-purine-isonucleoside
• nucleoside
• hepatitis C virus
• HCV

This work was supported in parts by the NIH grants 1R43 AI-52868 (biology) and 1R43AI-056720 (chemistry).

Notes

¹EC⁹⁰(μM) is a concentration that reduces 90% of the viral RNA in the replicon system cell.

²CC⁵⁰ (μM) is a concentration that reduces 50% of cellular mRNA in the replicon system cell.

³IC⁵⁰ (μM) is a concentration that reduces 50% of cellular growth.

⁴Not determined.