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Identification of 4-anilino-quin(az)oline as a cell active Protein Kinase Novel 3 (PKN3) inhibitor chemotype.

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Deep annotation of a library of 4-anilinoquinolines led to the identification of 7-iodo- N -(3,4,5-trimethoxyphenyl)quinolin-4-amine 16 as a potent inhibitor (IC 50 = 14 nM) of Protein Kinase Novel 3… Click to show full abstract

Deep annotation of a library of 4-anilinoquinolines led to the identification of 7-iodo- N -(3,4,5-trimethoxyphenyl)quinolin-4-amine 16 as a potent inhibitor (IC 50 = 14 nM) of Protein Kinase Novel 3 (PKN3) with micromolar activity in cells. Compound 16 is a potential tool compound to study the cell biology of PKN3 and its role in pancreatic and prostate cancer and T-cell acute lymphoblastic leukemia. These 4-anilinoquinolines may also be useful tools to uncover the therapeutic potential of PKN3 inhibition in a broad range of diseases.

Keywords: kinase novel; protein kinase; identification; cell; novel pkn3; inhibitor

Journal Title: ChemMedChem
Year Published: 2022

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