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Back-pocket optimization of 2-aminopyrimidine-based macrocycles leads to potent dual EPHA2/GAK kinase inhibitors with antiviral activity
Authors
Joshua Gerninghaus,Rezart Zhubi
Andreas Kraemer,Marwah Karim,Do Hoang Nhu Tran,Andreas C Joerger,Christian Schreiber,Lena M. Berger,Benedict Tilman Berger,Theresa A.L. Ehret,Lewis Elson,Christopher Lenz,Krishna Saxena,Susanne Mueller,Shirit Einav,Stefan Knapp,Thomas Hanke,Andreas Krämer,Tran Nhu,A.C. Joerger,Lena Berger,Benedict‐Tilman Berger,Theresa Ehret,Susanne Müller
+22 authors
,Do TranPublished
Feb 18, 2024
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Abstract
Macrocyclization of acyclic compounds is a powerful strategy for improving inhibitor potency and selectivity. Here, we developed a 2-aminopyrimidine-based macrocyclic dual EPHA2/GAK kinase inhibitor as a chemical tool to study the role of these two kinases in viral entry and assembly. Starting with a promiscuous macrocyclic inhibitor,
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