Discovery of potent nucleotide-mimicking competitive inhibitors of hepatitis C virus NS3 helicase

作者：Gemma Sandra; Butini Stefania; Campiani Giuseppe^*; Brindisi Margherita; Zanoli Samantha; Romano Maria Pia; Tripaldi Pierangela; Savini Luisa; Fiorini Isabella; Borrelli Giuseppe; Novellino Ettore; Maga Giovanni

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(9): 2776-2779.

DOI：10.1016/j.bmcl.2010.09.002

• HCV
• Helicase
• Hydrazides

Among the enzymes involved in the life cycle of HCV, the non-structural protein NS3, with its double function of protease and NTPase/helicase, is essential for the virus replication. Exploiting our previous knowledge in the development of nucleotide-mimicking NS3 helicase (NS3h) inhibitors endowed with key structural and electronic features necessary for an optimal ligand-enzyme interaction, we developed the tetrahydroacridinyl derivative 3a as the most potent NS3h competitive inhibitor reported to date (HCV NS3h K(i) = 20 nM).

• 出版日期2011-5-1