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Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2016

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

Résumé

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 (IC$_{50}$ of 0.7 $\mu$M) and DYRK1A (IC$_{50}$ of 2.6 $\mu$M).
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Dates et versions

hal-03875851 , version 1 (28-11-2022)

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Marie Lawson, Jordi Rodrigo, Blandine Baratte, Thomas Robert, Claire Delehouzé, et al.. Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2- a ]pyridines derivatives as protein kinase inhibitors. European Journal of Medicinal Chemistry, 2016, 123, pp.105 - 114. ⟨10.1016/j.ejmech.2016.07.040⟩. ⟨hal-03875851⟩
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