Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity
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.
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.
p. 3544 - 3549
(2012/06/18)
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