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  • Inhibition of hepatitis C replication by targeting the molecular chaperone Hsp90 - synthesis and biological evaluation of 4,5,6,7-tetrahydrobenzo[1,2-d]thiazole derivatives [Elektronski vir]
    Lillsunde, Katja-Emilia ...
    Cellular chaperones that belong to the heat-shock protein 90 (Hsp90) family are a prerequisite for successful viral propagation for most viruses. The hepatitis C virus (HCV) uses Hsp90 for ... maturation, folding and modification of viral proteins. Based on our previous discovery that marine alkaloid analogues with 4,5,6,7-tetrahydrobenzo[1,2-d]thiazole-2-amine structure show inhibition of HCV replication and potential binding to Hsp90, a series of twelve novel compounds based on this scaffold was designed and synthesized. The aim was improved Hsp90 affinity and anti-HCV activity. Through structural optimization, improved binding to Hsp90 and specific HCV inhibition in genotype 1b and 2a replicon models was achieved for compounds 2, 5 and 8. Furthermore, these compounds efficiently inhibited replication of full-length HCV genotype 2a in a reporter virus RNA assay with IC50-values ranging from 0.03 to 0.6 microM.
    Vir: ChemMedChem. - ISSN 1860-7187 (Vol. 14, iss. 3, 2019, str. 334-342)
    Vrsta gradiva - e-članek
    Leto - 2019
    Jezik - angleški
    COBISS.SI-ID - 4649585

    Povezava(-e):

    https://onlinelibrary.wiley.com/doi/pdf/10.1002/cmdc.201800724
    DOI

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