Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1362740 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Nathalie Bouloc, Jonathan M. Large, Magda Kosmopoulou, Chongbo Sun, Amir Faisal, Mizio Matteucci, Jóhannes Reynisson, Nathan Brown, Butrus Atrash, Julian Blagg, Edward McDonald, Spiros Linardopoulos, Richard Bayliss, Vassilios Bavetsias,