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ID: ALA4041550

Journal: ACS Med Chem Lett

Title: Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.

Authors: Liang Y, de Wispelaere M, Carocci M, Liu Q, Wang J, Yang PL, Gray NS.

Abstract: Here we report the structure-activity relationship (SAR) investigations of QL-XII-47 (QL47), a compound that possesses broad-spectrum antiviral activity against dengue virus and other RNA viruses. A medicinal chemistry campaign initiated from QL47, a previously reported covalent BTK inhibitor, to derive YKL-04-085, which is devoid of any kinase activity when screened against a panel of 468 kinases and with improved pharmacokinetic properties. Both QL47 and YKL-04-085 are potent inhibitors of viral translation and exhibit cellular antiviral activity at 35-fold lower concentrations relative to inhibition of host-cell proliferation.

CiteXplore: 28337328

DOI: 10.1021/acsmedchemlett.7b00008