TY - JOUR T1 - Identification and Optimization of cell active 4-anilino-quin(az)oline Inhibitors for Protein Kinase Novel 3 (PKN3) JF - bioRxiv DO - 10.1101/2020.03.02.972943 SP - 2020.03.02.972943 AU - Christopher R. M. Asquith AU - Louisa Temme AU - Tuomo Laitinen AU - Julie Pickett AU - Frank E. Kwarcinski AU - Parvathi Sinha AU - Carrow I. Wells AU - Graham J. Tizzard AU - Reena Zutshi AU - David H. Drewry Y1 - 2020/01/01 UR - http://biorxiv.org/content/early/2020/03/03/2020.03.02.972943.abstract N2 - The development of a small library of 4-anilinoquinolines led to the identification of 7-iodo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine 16 as a potent inhibitor of Protein Kinase Novel 3 (PKN3) with an IC50 of 1.3 μM in cells. Compound 16 presents a useful potential tool compound to study the biology of PKN3 including links to pancreatic and prostate cancer, along with T-cell acute lymphoblastic leukemia. These compounds may be useful tools to explore the therapeutic potential of PKN3 inhibition in prevention of a broad range of infectious and systemic diseases. ER -