Identification of 4‐Anilinoquin(az)oline as a Cell‐Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype
Deep annotation of a library of 4-anilinoquin(az)olines led to the identification of 7-iodo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine 16 as a potent inhibitor (IC<sub>50</sub> =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-anilinoquin(az)olines may also be useful tools to uncover the therapeutic potential of PKN3 inhibition in a broad range of diseases.
Authors
- Christopher R. M. Asquith (ORCID: https://orcid.org/0000-0001-5871-3458)
- Louisa Temme (ORCID: https://orcid.org/0000-0003-3753-4973)
- Julie E. Pickett (ORCID: https://orcid.org/0000-0002-9535-8528)
- Frank E. Kwarcinski
- Gary L. Johnson (ORCID: https://orcid.org/0000-0003-2867-0551)
- Reena Zutshi (ORCID: https://orcid.org/0000-0002-2582-1484)
- Tuomo Laitinen (ORCID: https://orcid.org/0000-0003-1539-2142)
- Parvathi Sinha
- Michael P. East (ORCID: https://orcid.org/0000-0002-1994-6117)
- Carrow I. Wells (ORCID: https://orcid.org/0000-0003-4799-6792)
- David H. Drewry (ORCID: https://orcid.org/0000-0001-5973-5798)
Institutions
- University of North Carolina at Chapel Hill (US)
Publication Details
- Journal
- UNC Libraries
- Published
- 2025-10-10
- DOI
- https://doi.org/10.17615/rnrw-0310
- Primary Topic
- Synthesis and biological activity
- Type
- article
- Field-Weighted Citation Impact
- 0.00