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

Author(s): Yang Liu, Yijing Li, Jianzhen Liu, Limin Yang, Pengzhan Li, Guisen Zhao

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 4 , 2016

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Abstract:

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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Article Details

VOLUME: 13
ISSUE: 4
Year: 2016
Page: [314 - 323]
Pages: 10
DOI: 10.2174/1570180812666150819003111
Price: $65

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