445264-23-3Relevant academic research and scientific papers
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells
Bouloc, Nathalie,Large, Jonathan M.,Kosmopoulou, Magda,Sun, Chongbo,Faisal, Amir,Matteucci, Mizio,Reynisson, Jóhannes,Brown, Nathan,Atrash, Butrus,Blagg, Julian,McDonald, Edward,Linardopoulos, Spiros,Bayliss, Richard,Bavetsias, Vassilios
scheme or table, p. 5988 - 5993 (2010/11/02)
Co-crystallisation of the imidazo[1,2-a]pyrazine derivative 15 (3-chloro-N-(4-morpholinophenyl)-6-(pyridin-3-yl)imidazo[1,2-a]pyrazin-8-amine) with Aurora-A provided an insight into the interactions of this class of compound with Aurora kinases. This led to the design and synthesis of potent Aurora-A inhibitors demonstrating up to 70-fold selectivity in cell-based Aurora kinase pharmacodynamic biomarker assays.
