Design, Synthesis, and Evaluation of the Kinase Inhibition Potential of Pyridylpyrimidinylaminophenyl Derivatives

In view of potent kinase inhibitors for the treatment of myriad human disorders, we synthesized some structurally variant amide/cyclic amide derivatives based on pyridylpyrimidinylaminophenyl amine, the key pharmacophore of the kinase inhibitor drug molecule, imatinib, and evaluated their kinase inhibition potency. Among the various synthesized amides, compound 20 , a cyclic amide/pyridin‐2(1 H )‐one derivative, exhibited an IC 50 value comparable to that of the drug imatinib against c‐Src kinase, and another compound ( 14 ) containing a 2‐((4‐methyl‐2‐oxo‐2 H ‐chromen‐6‐yl)oxy)acetamide demonstrated an IC 50 value of 8.39 μM. Furthermore, the constitution of the cyclic amide derivative was confirmed by the single‐crystal X‐ray diffraction technique. These results may serve as a gateway for developing novel next‐generation kinase inhibitors.