Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity |
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Authors: | Voss Matthew E Rainka Matthew P Fleming Mike Peterson Lisa H Belanger David B Siddiqui M Arshad Hruza Alan Voigt Johannes Gray Kimberly Basso Andrea D |
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Institution: | AMRI Global, 26 Corporate Circle, Albany, NY 12212, USA. matthew.voss@amriglobal.com |
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Abstract: | The structure-activity relationships of new Aurora A/B kinase inhibitors derived from the previously identified kinase inhibitor 12 are described. Introduction of acetic acid amides onto the pyrazole of compound 12 was postulated to influence Aurora A/B selectivity and improve the profile against off-target kinases. The SAR of the acetic acid amides was explored and the effect of substitution on enzyme inhibition as well as mechanism-based cell activity was studied. Additionally, several of the more potent inhibitors were screened for their off-target kinase selectivity. |
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