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  • Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors.

Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors.

European journal of medicinal chemistry (2016-07-31)
Marie Lawson, Jordi Rodrigo, Blandine Baratte, Thomas Robert, Claire Delehouzé, Olivier Lozach, Sandrine Ruchaud, Stéphane Bach, Jean-Daniel Brion, Mouad Alami, Abdallah Hamze
RESUMO

We report here the synthesis, the biological evaluation and the molecular modeling studies of new imidazo[1,2-a]pyridines derivatives designed as potent kinase inhibitors. This collection was obtained from 2-aminopyridines and 2-bromoacetophenone which afforded final compound in only one step. The bioactivity of this family of new compounds was tested using protein kinase and ATP competition assays. The structure-activity relationship (SAR) revealed that six compounds inhibit DYRK1A and CLK1 at a micromolar range. Docking studies provided possible explanations that correlate with the SAR data. The most active compound 4c inhibits CLK1 (IC50 of 0.7 μM) and DYRK1A (IC50 of 2.6 μM).

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Casein, Dephosphorylated from bovine milk, lyophilized powder