The Aurora kinases are serine/threonine kinases that regulate key mitotic events and are emerging as attractive targets for anti-cancer drug development.  Our continued effort towards development of the imidazo[1,2-a]pyrazine scaffold as Aurora kinase inhibitors is described.  Bioisosteric approach was applied to optimize the 8-position of the scaffold.  The synthesis and structure-activity relationships (SAR) will be discussed.

From isothiazole to thiophene and thiazole:  A bioisosteric approach to the discovery of potent imidazo[1,2-a]pyrazines as Aurora kinase inhibitors

240th National Meeting (2010)

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