Martinez-Gonzalez, Sonia published the artcileDiscovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors, COA of Formula: C10H20N2O2, the main research area is triazolopyridazinylquinoline derivative PIM kinase inhibition antiproliferative anticancer; Anticancer agents; Antiproliferative activity; Chemical probes; PIM-1 inhibitors; Selective PIM-1/PIM-3 inhibitors; Synergistic effects; pan-PIM inhibitors.
PIM kinase family (PIM-1, PIM-2 and PIM-3) is an appealing target for the discovery and development of selective inhibitors, useful in various disease conditions in which these proteins are highly expressed, such as cancer. The significant effort put, in the recent years, towards the development of small mols. exhibiting inhibitory activity against this protein family has ended up with several mols. entering clin. trials. As part of our ongoing exploration for potential drug candidates that exhibit affinity towards this protein family, we have generated a novel chem. series of triazolo[4,3-b]pyridazine based tricycles by applying a scaffold hopping strategy over our previously reported potent pan-PIM inhibitor ETP-47453 (compound 2). The structure-activity relationship studies presented herein demonstrate a rather selective PIM-1/PIM-3 biochem. profile for this novel series of tricycles, although pan-PIM and PIM-1 inhibitors have also been identified. Selected examples show significant inhibition of the phosphorylation of BAD protein in a cell-based assay. Moreover, optimized and highly selective compounds, such as 42, did not show significant hERG inhibition at 20 μM concentration, and proved its antiproliferative activity and utility in combination with particular antitumoral agents in several tumor cell lines.
European Journal of Medicinal Chemistry published new progress about Acute myeloid leukemia. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, COA of Formula: C10H20N2O2.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem