Bendjeddou, Lyamin Z.; Loaec, Nadege; Villiers, Benoit; Prina, Eric; Spath, Gerald F.; Galons, Herve; Meijer, Laurent; Oumata, Nassima published the artcile< Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor>, Category: esters-buliding-blocks, the main research area is imidazopyridazine preparation antileishmanial cytotoxicity protein kinase inhibitor human; CLKs; Imidazo[1,2-b]pyridazine; Kinase inhibitor; Leishmania, DYRK1A; Unicellular parasites.
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 < 100 nM. The characterization of the kinome of several parasites, such as Plasmodium and Leishmania, has pointed out profound divergences between protein kinases of the parasites and those of the host. The activities of the prepared compounds against 11 parasitic kinases was investigated. 3,6-Disubstituted imidazo[1,2-b]pyridazines showed potent inhibition of Plasmodium falciparum CLK1 (PfCLK1). Compound I was found to be the most selective product against CLK1 (IC50 = 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. European Journal of Medicinal Chemistry published new progress about Cytotoxicity. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.
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