Potent and selective inhibitors of the Abl-kinase: Phenylaminopyrimidine (PAP) derivatives

Article abstract of DOI:10.1016/S0960-894X(96)00601-4

Due to its relatively clear etiology, chronic myelogenous leukemia (CML) represents an ideal disease target for a therapy using a selective inhibitor of the Bcr-Abl tyrosine protein kinase. Extensive optimization of the class of phenylamino-pyrimidines yielded highly potent and selective Bcr-Abl kinase inhibitors. Compound 1 shows high potency (IC₅₀ = 38 nM) and selectivity for the Abl tyrosine protein kinase at the in vitro level.