Blocking epidermal growth factor receptor (EGFR) has been the hotspot in the field of cancer
therapy. Based on the fact that salicylanilides possess well inhibitory activity against EGFR tyrosine
kinase, a series of salicylamide analogs bearing 4’-substitution were designed to explore new
candidates exhibiting improved efficacy against EGFR. Many of the synthesized compounds inhibited
EGFR in the micromolar range, especially compounds 15a and 15b (IC50 = 0.27 μM and 1.1μM, respectively). We report
our findings as a basis for further development in salicylamide analogues as EGFR inhibitors.
Keywords: EGFR inhibitors, in vitro enzyme assay, synthesis, molecular modeling, salicylamides, structure–activity relationships.
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