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

作　　者：Ning Ding Wei Zhang Hua Ling Xiao Peng Wang Ying Xia Li 

机构地区：[1]Department of Medicinal Chemistry,School of Pharmacy,Fudan University,Shanghai 201203,China [2]School of Medicine and Pharmacy,Ocean University of China,Qingdao 266003,China

出　　处：《Chinese Chemical Letters》2012年第5期529-532,共4页中国化学快报（英文版）

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)

摘　　要：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）.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）.

关 键 词：Salicylanilides EGFR HER2 Tyrosine kinase inhibitor 

分 类 号：TQ463.54[化学工程—制药化工] Q55[生物学—生物化学]