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Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines. Bioorganic & medicinal chemistry letters Saul, S., Pu, S., Zuercher, W. J., Einav, S., Asquith, C. R. 2020; 30 (16): 127284

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=79nM. Crucially, these compounds showed very limited toxicity with CC50 values >10M in almost all cases. This new promising series provides an anchor point for further development to optimize compound properties.

View details for DOI 10.1016/j.bmcl.2020.127284

View details for PubMedID 32631507