Design, synthesis and biological evaluation of salicylamide analogues as epidermal growth factor receptor tyrosine kinase inhibitors

Yang Liu; Yijing Li; Jianzhen Liu; Limin Yang; Pengzhan Li; Guisen Zhao

doi:10.2174/1570180812666150819003111

Design, synthesis and biological evaluation of salicylamide analogues as epidermal growth factor receptor tyrosine kinase inhibitors

Yang Liu, Yijing Li, Jianzhen Liu, Limin Yang, Pengzhan Li, Guisen Zhao

Research output: Contribution to journal › Article › peer-review

1 Scopus citations

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.

Original language	English (US)
Pages (from-to)	314-323
Number of pages	10
Journal	Letters in Drug Design and Discovery
Volume	13
Issue number	4
DOIs	https://doi.org/10.2174/1570180812666150819003111
State	Published - Apr 1 2016
Externally published	Yes

Keywords

EGFR inhibitors
In vitro enzyme assay
Molecular modeling
Salicylamides
Structure-activity relationships
Synthesis

ASJC Scopus subject areas

Molecular Medicine
Pharmaceutical Science
Drug Discovery

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10.2174/1570180812666150819003111

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title = "Design, synthesis and biological evaluation of salicylamide analogues as epidermal growth factor receptor tyrosine kinase inhibitors",

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.",

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T1 - Design, synthesis and biological evaluation of salicylamide analogues as epidermal growth factor receptor tyrosine kinase inhibitors

AU - Liu, Yang

AU - Li, Yijing

AU - Liu, Jianzhen

AU - Yang, Limin

AU - Li, Pengzhan

AU - Zhao, Guisen

PY - 2016/4/1

Y1 - 2016/4/1

N2 - 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.

AB - 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.

KW - EGFR inhibitors

KW - In vitro enzyme assay

KW - Molecular modeling

KW - Salicylamides

KW - Structure-activity relationships

KW - Synthesis

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Design, synthesis and biological evaluation of salicylamide analogues as epidermal growth factor receptor tyrosine kinase inhibitors

Abstract

Keywords

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