Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors

Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors

[Display omitted] A series of novel morpholin-3-one-fused quinazoline derivatives were designed, synthesized and evaluated as EGFR tyrosine kinase inhibitors. Nineteen compounds showed significant inhibitory activities against EGFRwt kinase (IC50

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2016-03, Vol.26 (6), p.1571-1575
Hauptverfasser: Qin, Xuemei, Lv, Yongjuan, Liu, Peng, Li, Zhipeng, Hu, Liming, Zeng, Chengchu, Yang, Leifu
Format: Artikel
Sprache:eng
Schlagworte:
Anti-cancer
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cell Line, Tumor
Cell Proliferation - drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
EGFR inhibitors
Humans
Molecular docking
Molecular Docking Simulation
Molecular Structure
Morpholines - chemistry
Morpholines - pharmacology
NSCLC
Protein Kinase Inhibitors - chemical synthesis
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacology
Quinazoline
Quinazolines - chemistry
Quinazolines - pharmacology
Receptor, Epidermal Growth Factor - antagonists & inhibitors
Receptor, Epidermal Growth Factor - metabolism
Structure-Activity Relationship
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Zusammenfassung:[Display omitted] A series of novel morpholin-3-one-fused quinazoline derivatives were designed, synthesized and evaluated as EGFR tyrosine kinase inhibitors. Nineteen compounds showed significant inhibitory activities against EGFRwt kinase (IC50
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2016.02.009