| Literature DB >> 25248682 |
Amélie Bruel1, Romain Bénéteau1, Mylène Chabanne1, Olivier Lozach2, Rémy Le Guevel3, Myriam Ravache3, Hélène Bénédetti4, Laurent Meijer5, Cédric Logé6, Jean-Michel Robert1.
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.Entities:
Keywords: 4-Oxo-3,4-dihydro-5H-pyridazino[4,5-b]indole; Anti-proliferative effects; DYRK1A inhibitors; Pyridazin-3(2H)-one; Synthesis
Mesh：
Substances：
Year: 2014 PMID： 25248682 DOI： 10.1016/j.bmcl.2014.09.017
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823