Synthesis and SAR studies of imidazo-[1, 2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity

ME Voss, MP Rainka, M Fleming, LH Peterson…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 10 p. 3544 - 3549

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Citation Number: 10

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 ...