Discovery of a novel tricyclic 4H-thiazolo[5′,4′:4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity
2015
Abstract A novel, previously undescribed 4 H -thiazolo[5′,4′:4,5]pyrano[2,3- c ]pyridine tricyclic scaffold has been discovered. The application of this novel chemotype leading to a potent and selective prototype PI3Kα inhibitor with favorable physicochemical and PK-properties is described.
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