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Title: Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.
Authors: Bouloc, N
Large, JM
Kosmopoulou, M
Sun, C
Faisal, A
Matteucci, M
Reynisson, J
Brown, N
Atrash, B
Blagg, J
McDonald, E
Linardopoulos, S
Bayliss, R
Bavetsias, V
First Published: 15-Oct-2010
Citation: BIOORG MED CHEM LETT, 2010, 20 (20), pp. 5988-5993
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.
DOI Link: 10.1016/j.bmcl.2010.08.091
eISSN: 1464-3405
Type: Journal Article
Appears in Collections:Published Articles, Dept. of Biochemistry

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