Design, Synthesis and Biological Evaluation of Salicylamide Analogues as Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors

被引：1

作者：

Liu, Yang ^{[1
]}

Li, Yijing ^{[2
]}

Liu, Jianzhen ^{[1
]}

Yang, Limin ^{[3
]}

Li, Pengzhan ^{[1
]}

Zhao, Guisen ^{[1
]}

机构：

[1] Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Key Lab Chem Biol,Minist Educ, Jinan 250012, Shandong, Peoples R China

[2] Binzhou Ctr Food & Drug Control, Binzhou 256618, Shandong, Peoples R China

[3] Xinxiang Med Univ, Sch Pharm, Xinxiang 453003, Henan, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2016年 / 13卷 / 04期

关键词：

EGFR inhibitors; in vitro enzyme assay; synthesis; molecular modeling; salicylamides; structure-activity relationships; DUAL INHIBITORS; EGFR; LAPATINIB; SCAFFOLD; CANCER; CELLS;

D O I：

10.2174/1570180812666150819003111

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 mu M and 1.1 mu M, respectively). We report our findings as a basis for further development in salicylamide analogues as EGFR inhibitors.

引用

页码：314 / 323

页数：10

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