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Beilstein J. Org. Chem. 2025, 21, 2250–2259, doi:10.3762/bjoc.21.172
Graphical Abstract
Figure 1: A) Sequence of amino acids in CLK3 as compared to the three other CLKs; B) Structure of CLK3 highli...
Figure 2: A) Docking of our previous inhibitor (DB18) in CLK3 and B) our working hypothesis.
Figure 3: Design of our target molecules.
Scheme 1: Synthesis of the intermediate anilino-2-quinazolines 7a and 7b.
Scheme 2: Synthesis of the targeted anilino-2-quinazolines 10 and 13.
Figure 4: Primary evaluation of the inhibition of the new quinazolines against a short panel of mammalian kin...
Figure 5: Docking of VS-77 in CLK3.
Figure 6: Docking of VS-77 in Hs_DYRK1A (PDB ID: 8T2H [26]).