928336-89-4Relevant academic research and scientific papers
Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor
Bendjeddou, Lyamin Z.,Loa?c, Nadège,Villiers, Beno?t,Prina, Eric,Sp?th, Gerald F.,Galons, Hervé,Meijer, Laurent,Oumata, Nassima
, p. 696 - 709 (2017)
3,6-Disubstituted imidazo[1,2-b]pyridazine derivatives were synthesized to identify new inhibitors of various eukaryotic kinases, including mammalian and protozoan kinases. Among the imidazo[1,2-b]pyridazines tested as kinase inhibitors, several derivatives were selective for DYRKs and CLKs, with IC50?50?=?82?nM), CLK4 (IC50?=?44?nM), DYRK1A (IC50?=?50?nM), and PfCLK1 (IC50?=?32?nM). The compounds were also tested against Leishmania amazonensis. Several compounds showed anti-leishmanial activity at rather high (10?μM) concentration, but were not toxic at 1?μM or 10?μM, as judged by viability assays carried out using a neuroblastoma cell line.
