Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors.
Basic Information
ID: ALA3351708
Journal: Bioorg Med Chem Lett
Title: Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors.
Authors: Bruel A, Bénéteau R, Chabanne M, Lozach O, Le Guevel R, Ravache M, Bénédetti H, Meijer L, Logé C, Robert JM.
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.
CiteXplore: 25248682
DOI: 10.1016/j.bmcl.2014.09.017
Patent ID: ┄