Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors

Abstract : New pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs were synthesized and their inhibitory activities against DYRK1A, CDK5/p25, GSK3α/β and p110-α isoform of PI3K evaluated using harmine as reference. Both furan-2-yl 10 and pyridin-4-yl 19 from the two different series, exhibited submicromolar IC50 against DYRK1A with no activities against the three other kinases. In addition, compound 10 exhibited antiproliferative activities in the Huh-7, Caco2 and MDA-MB-231 cell lines.
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Amélie Bruel, Romain Bénéteau, Mylène Chabanne, Olivier Lozach, Rémy Le Guevel, et al.. Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2014, 24 (21), pp.5037 - 5040. ⟨10.1016/j.bmcl.2014.09.017⟩. ⟨hal-01086026⟩

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