Macrocyclization of Broad-Spectrum Kinase Inhibitor Bosutinib leads to Potent and Selective Quinoline-based HIPK4 Inhibitor AZ137
Athina Zerva, Nicolai D. Raig, Zaile Zhuang, Andreas Kraemer, Johannes Dopfer, Riley K. Togashi, Martin P. Schwalm, Lewis Elson, Julia Marie Frischkorn, Benedict‐Tilman Berger, Susanne Müller, James Chen, Stefan Knapp, Thomas Hanke
The paper describes the development of AZ137, a potent and selective HIPK4 inhibitor derived from bosutinib, and validates its utility as a tool for studying HIPK4's biological functions.
Journal of Medicinal Chemistry · Aug 18, 2026Peer-reviewedBiochemistry