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 ...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±1.265μmol/L）.展开更多
基金supported by the Research Fund for the Doctoral Program of Higher Education of China(No 20100071120051)the Fundamental Research Funds for the Central Universities(No10FX061)
文摘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±1.265μmol/L）.
