1239441-53-2Relevant academic research and scientific papers
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases
Matthews, Thomas P.,McHardy, Tatiana,Klair, Suki,Boxall, Kathy,Fisher, Martin,Cherry, Michael,Allen, Charlotte E.,Addison, Glynn J.,Ellard, John,Aherne, G. Wynne,Westwood, Isaac M.,Montfort, Rob van,Garrett, Michelle D.,Reader, John C.,Collins, Ian
scheme or table, p. 4045 - 4049 (2010/08/19)
A range of 3,6-di(hetero)arylimidazo[1,2-a]pyrazine ATP-competitive inhibitors of CHK1 were developed by scaffold hopping from a weakly active screening hit. Efficient synthetic routes for parallel synthesis were developed to prepare analogues with improved potency and ligand efficiency against CHK1. Kinase profiling showed that the imidazo[1,2-a]pyrazines could inhibit other kinases, including CHK2 and ABL, with equivalent or better potency depending on the pendant substitution. These 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines appear to represent a general kinase inhibitor scaffold.
