Bioorganic and Medicinal Chemistry Letters p. 187 - 192 (1997)
Update date:2022-07-30
Topics: Inhibitors Selectivity Derivatives Potency Selective Inhibitors Potent Abl-kinase Phenylaminopyrimidine (PAP) derivatives
Zimmermann, Juerg
Buchdunger, Elisabeth
Mett, Helmut
Meyer, Thomas
Lydon, Nicholas B.
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.
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