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      Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines.

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          Abstract

          Screening a series of 4-anilinoquinolines and 4-anilinoquinazolines enabled identification of potent novel inhibitors of dengue virus (DENV). Preparation of focused 4-anilinoquinoline/quinazoline scaffold arrays led to the identification of a series of high potency 6-substituted bromine and iodine derivatives. The most potent compound 6-iodo-4-((3,4,5-trimethoxyphenyl)amino)quinoline-3-carbonitrile (47) inhibited DENV infection with an EC50 = 79 nM. Crucially, these compounds showed very limited toxicity with CC50 values >10 µM in almost all cases. This new promising series provides an anchor point for further development to optimize compound properties.

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          Author and article information

          Journal
          Bioorg Med Chem Lett
          Bioorganic & medicinal chemistry letters
          Elsevier BV
          1464-3405
          0960-894X
          August 15 2020
          : 30
          : 16
          Affiliations
          [1 ] Department of Medicine, Division of Infectious Diseases and Geographic Medicine, and Department of Microbiology and Immunology, Stanford University School of Medicine, Stanford, CA 94305, USA.
          [2 ] Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
          [3 ] Department of Medicine, Division of Infectious Diseases and Geographic Medicine, and Department of Microbiology and Immunology, Stanford University School of Medicine, Stanford, CA 94305, USA. Electronic address: seinav@stanford.edu.
          [4 ] Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA; Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA. Electronic address: chris.asquith@unc.edu.
          Article
          S0960-894X(20)30394-2
          10.1016/j.bmcl.2020.127284
          32631507
          ff22fedc-58df-475c-a4bc-3a3e11c67b30

          Flavivirus,4-Anilinoquinoline,Antiviral,4-Anilinoquinazoline,Dengue Virus

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