Identification and Optimization of cell active 4-anilino-quin(az)oline Inhibitors for Protein Kinase Novel 3 (PKN3)

Asquith, C. R. M.; Temme, L.; Laitinen, T.; Pickett, J.; Kwarcinski, F. E.; Sinha, P.; Wells, C. I.; Tizzard, G. J.; Zutshi, R.; Drewry, D. H.

doi:10.1101/2020.03.02.972943

bioRxiv · 10.1101/2020.03.02.972943

Identification and Optimization of cell active 4-anilino-quin(az)oline Inhibitors for Protein Kinase Novel 3 (PKN3)

Asquith, C. R. M.·Temme, L.·Laitinen, T.·Pickett, J.·Kwarcinski, F. E.·Sinha, P.·Wells, C. I.·Tizzard, G. J.·Zutshi, R.·Drewry, D. H.

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Abstract

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 M 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.

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Asquith, C. R. M., Temme, L., Laitinen, T., Pickett, J., Kwarcinski, F. E., Sinha, P., Wells, C. I., Tizzard, G. J., Zutshi, R., Drewry, D. H.. 2020-03-03. Identification and Optimization of cell active 4-anilino-quin(az)oline Inhibitors for Protein Kinase Novel 3 (PKN3). https://doi.org/10.1101/2020.03.02.972943

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