| Literature DB >> 20880703 |
Sandra Gemma1, Stefania Butini, Giuseppe Campiani, Margherita Brindisi, Samantha Zanoli, Maria Pia Romano, Pierangela Tripaldi, Luisa Savini, Isabella Fiorini, Giuseppe Borrelli, Ettore Novellino, Giovanni Maga.
Abstract
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).Entities:
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Year: 2010 PMID： 20880703 DOI： 10.1016/j.bmcl.2010.09.002
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823