Studies on the anti-hepatitis C virus activity of newly synthesized tropolone derivatives: identification of NS3 helicase inhibitors that specifically inhibit subgenomic …

…, M Bretner, AM Boguszewska-Chachulska

Index: Najda-Bernatowicz, Andelika; Krawczyk, Mariusz; Stankiewicz-Drogon, Anna; Bretner, Maria; Boguszewska-Chachulska, Anna M. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 14 p. 5129 - 5136

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Citation Number: 21

Abstract

We synthesized new tropolone derivatives substituted with cyclic amines: piperidine, piperazine or pyrrolidine. The most active anti-helicase compound (IC50= 3.4 μM), 3, 5, 7-tri [(4′-methylpiperazin-1′-yl) methyl] tropolone (2), inhibited RNA replication by 50% at 46.9 μM (EC50) and exhibited the lowest cytotoxicity (CC50)> 1mM resulting in a selectivity index (SI= CC50/EC50)> 21. The most efficient replication inhibitor, 3, 5, 7-tri [(4′- ...