Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.
Chemistry has been developed to access both imidazo[1,2-a]pyrazines and imidazo[1,2-c]pyrimidines. Small structural modifications in both series led to a switch of potency between two kinases involved in mediating cell cycle checkpoint control, CHK1 and MK2.
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GENE-Y CHEMICAL CHEMICAL CHEMICAL CHEMICAL GENE-N GENE-Y GENE-Y GENE-N GENE-Y
MK2 imidazo[1,2-a]pyrazines imidazo[1,2-c]pyrimidines imidazo[1,2-a]pyrazine imidazo[1,2-c]pyrimidine kinases CHK1 MK2 kinase CHK1