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

Add time:08/21/2019    Source:sciencedirect.com

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).

We also recommend Trading Suppliers and Manufacturers of ETHYL (5-BROMOIMIDAZO[1,2-A]PYRIDIN-2-YL)ACETATE (cas 135995-46-9). Pls Click Website Link as below: cas 135995-46-9 suppliers

Prev:Research paperDesign, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors
Next:Spatial Structure of Zervamicin IIB Bound to DPC Micelles: Implications for Voltage-Gating)