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© Jean-Claude Antoine
Leishmania mexicana amazonensis
Publication : European journal of medicinal chemistry

Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in European journal of medicinal chemistry - 22 Sep 2016

Bendjeddou LZ, Loaëc N, Villiers B, Prina E, Späth GF, Galons H, Meijer L, Oumata N

Link to Pubmed [PMID] – 27721154

Eur J Med Chem 2017 Jan;125:696-709

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 IC < 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. This led us to investigate the activities of the prepared compounds against 11 parasitic kinases. 3,6-Disubstituted imidazo[1,2-b]pyridazines showed potent inhibition of Plasmodium falciparum CLK1 (PfCLK1). Compound 20a was found to be the most selective product against CLK1 (IC = 82 nM), CLK4 (IC = 44 nM), DYRK1A (IC = 50 nM), and PfCLK1 (IC = 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.

https://www.ncbi.nlm.nih.gov/pubmed/27721154