%0 Journal Article %T Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors %+ Cibles et Médicaments des Infections et de l'Immunité (IICiMed) %+ Phophorylation de protéines et Pathologies Humaines (P3H) %+ Génétique fonctionnelle, agronomie et santé [IFR 140] (GFAS) %+ Centre de biophysique moléculaire (CBM) %+ ManRos Therapeutics %A Bruel, Amélie %A Bénéteau, Romain %A Chabanne, Mylène %A Lozach, Olivier %A Le Guevel, Rémy %A Ravache, Myriam %A Bénédetti, Hélène %A Meijer, Laurent %A Logé, Cédric %A Robert, Jean-Michel %Z This work was supported by grant from the Cancéropôle Grand Ouest. %< avec comité de lecture %@ 0960-894X %J Bioorganic and Medicinal Chemistry Letters %I Elsevier %V 24 %N 21 %P 5037 - 5040 %8 2014-11 %D 2014 %R 10.1016/j.bmcl.2014.09.017 %K 4-Oxo-3 %K 4-dihydro-5H-pyridazino[4 %K 5-b]indole %K Pyridazin-3(2H)-one %K DYRK1A inhibitors %K Anti-proliferative effects %K Synthesis %Z Life Sciences [q-bio]/Biochemistry, Molecular Biology/Biochemistry [q-bio.BM]Journal articles %X 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. %G English %2 https://univ-rennes.hal.science/hal-01086026/document %2 https://univ-rennes.hal.science/hal-01086026/file/Synthesis%20of%20new%20pyridazino_accepted.pdf %L hal-01086026 %U https://univ-rennes.hal.science/hal-01086026 %~ UNIV-NANTES %~ UPMC %~ UNIV-RENNES1 %~ CNRS %~ UNIV-ORLEANS %~ INRA %~ IFR140 %~ CBM %~ LBI2M %~ P3H %~ STATS-UR1 %~ INC-CNRS %~ UR1-HAL %~ AGREENIUM %~ UPMC_POLE_3 %~ TEST-UNIV-RENNES %~ TEST-UR-CSS %~ UNIV-RENNES %~ SORBONNE-UNIVERSITE %~ SU-SCIENCES %~ SU-SCI %~ INRAE %~ SU-TI %~ ALLIANCE-SU %~ IICIMED %~ NANTES-UNIVERSITE %~ UNIV-NANTES-AV2022 %~ TEST2-HALCNRS %~ TEST3-HALCNRS %~ SBR