Synthesis and biological evaluation of a series of novel salicylanilides as inhibitors of EGFR protein tyrosine kinases

Abstract The synthesis and biological evaluation of two series of salicylanilide derivatives on the EGFR and ErbB-2 tyrosine kinases inhibitory activities were conducted. Of the tested compounds those having an additional aryl group substituted on the anilino ring were active on the EGFR tyrosine kinase inhibition ( 7a – c and 13a , 13c , 13d , 13f ). The inhibitory activities were all in the low micromolar or submicromolar range. In addition, compound 13a was found to have dual inhibitory activities both on EGFR and ErbB-2 tyrosine kinases (1.654 ± 1.280 and 7.134 ± 1.265 μmol/L).