Abstract
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(1H)-one derivative, exhibited an IC50 value comparable to that of the drug imatinib against c-Src kinase, and another compound (14) containing a 2-((4-methyl-2-oxo-2H-chromen-6-yl)oxy)acetamide demonstrated an IC50 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.
Original language | English (US) |
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Article number | 1600390 |
Journal | Archiv der Pharmazie |
Volume | 350 |
Issue number | 3-4 |
DOIs | |
State | Published - Apr 1 2017 |
Keywords
- Amide derivatives
- Imatinib
- Kinase inhibitors
- Pyridin-2(1H)-one
- Pyridylpyrimidinylaminophenyl
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery