Novel oxazolo[4,5-g]quinazolin-2(1H)-ones: Dual inhibitors of EGFR and Src protein tyrosine kinases

• Published in: European journal of medicinal chemistry Vol. 55; pp. 39 - 48
• Main Authors: Lin, Jinsheng, Shen, Wei, Xue, Jingwei, Sun, Juan, Zhang, Xue, Zhang, Can
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 01.09.2012; Elsevier
• Subjects: Anti-tumor agents; Biological and medical sciences; Cell Line, Tumor; Cell Proliferation - drug effects; Chemistry, Medicinal; EGFR inhibitor; Humans; Life Sciences & Biomedicine; Medical sciences; Miscellaneous; Molecular Docking Simulation; Oxazolo[4,5-g]quinazolin-2(1H)-one scaffold; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Protein Conformation; Protein Kinase Inhibitors - chemical synthesis; Protein Kinase Inhibitors - chemistry; Protein Kinase Inhibitors - metabolism; Protein Kinase Inhibitors - pharmacology; Protein tyrosine kinases (PTK); Quinazolines - chemical synthesis; Quinazolines - chemistry; Quinazolines - metabolism; Quinazolines - pharmacology; Receptor, Epidermal Growth Factor - antagonists & inhibitors; Receptor, Epidermal Growth Factor - chemistry; Receptor, Epidermal Growth Factor - metabolism; Science & Technology; Src inhibitor; src-Family Kinases - antagonists & inhibitors; src-Family Kinases - chemistry; src-Family Kinases - metabolism; Protein tyrosine kinases (PTK); Src inhibitor; Anti-tumor agents; Oxazolo[4,5-g]quinazolin-2(1H)-one scaffold; EGFR inhibitor; NNLYOFSWWFKIMS-UHFFFAOYSA-N; IRREVERSIBLE INHIBITORS; CANCER; GROWTH-FACTOR RECEPTOR; NEUTRAL 5-SUBSTITUTED 4-ANILINOQUINAZOLINES; POTENT; ORALLY-ACTIVE INHIBITORS; EXPRESSION; BINDING; Oxazolo[4,5-g]quinazolin-2(1H)-one; scaffold

Quinazoline-containing derivatives are an important class of synthetic products and represent an attractive scaffold for EGFR inhibitors. A series of oxazolo[4,5-g]quinazolin-2(1H)-one derivatives were synthesized and the EGFR and Src inhibition activities were evaluated using Gefitinib as lead comp...