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Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series |
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| Authors: | Barlaam Bernard Ducray Richard Lambert-van der Brempt Christine Plé Patrick Bardelle Catherine Brooks Nigel Coleman Tanya Cross Darren Kettle Jason G Read Jon |
| Institution: | a AstraZeneca, Centre de Recherches, Z.I. la Pompelle, BP1050, 51689 Reims, Cedex 2, France b AstraZeneca, Mereside, Alderley Park, Macclesfield SK10 4TG, UK |
| Abstract: | Optimization of our bis-anilino-pyrimidine series of EphB4 kinase inhibitors led to the discovery of compound 12 which incorporates a key m-hydroxymethylene group on the C4 aniline. 12 displays a good kinase selectivity profile, good physical properties and pharmacokinetic parameters, suggesting it is a suitable candidate to investigate the therapeutic potential of EphB4 kinase inhibitors. |
| Keywords: | EphB4 kinase Kinase inhibitor Bis-anilinopyrimidine |
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