Design, Synthesis and Biological Evaluation of 4-Arylamino-pyrimidine Derivatives As Focal Adhesion Kinase Inhibitors.
BIOORGANIC CHEMISTRY(2023)
摘要
•4-Arylamino-pyrimidine derivatives were designed and synthesized as new FAK inhibitors.•Compounds 8d and 9b exhibited potent activities against U87-MG cells with IC50 values of 0.975 μM, 1.033 μM, and FAK kinase with IC50 values of 0.2438 nM, 0.2691 nM.•Compounds 8d and 9b could induce U87-MG cell early apoptosis and arrest the cell at G2/M phase.•Compounds 8d and 9b could significantly inhibit U87-MG cell migration and clone formation.
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关键词
Antitumor,FAK inhibitor,Pyrimidine,Thiophene
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