- Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells
-
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.
- 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)
-
- IMIDAZO[1,2-A]PYRAZIN-8-YLAMINES AND METHOD OF INHIBITION OF BRUTON’S TYROSINE KINASE BY SUCH COMPOUNDS
-
Compounds of Formula (I-a) and all pharmaceutically-acceptable forms thereof, are described herein. The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined herein. Pharmaceutical compositions con
- -
-
Page/Page column 45
(2010/02/10)
-