Synthesis, Antitumor Evaluation and Docking Study of Novel 4-Anilinoquinazoline Derivatives as Potential Epidermal Growth Factor Receptor (EGFR) Inhibitors

• Published in: ChemMedChem Vol. 8; no. 6; pp. 928 - 933
• Main Authors: Rao, Guo-Wu, Xu, Geng-Jie, Wang, Jian, Jiang, Xu-Liang, Li, Hai-Bo
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 01.06.2013; WILEY‐VCH Verlag; Wiley; Wiley Subscription Services, Inc
• Subjects: 4-anilinoquinazolines; Aniline Compounds - chemical synthesis; Aniline Compounds - chemistry; Aniline Compounds - pharmacology; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; antitumor agents; Cell Line, Tumor; Cell Proliferation - drug effects; Chemistry, Medicinal; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; epidermal growth factor receptor (EGFR); Humans; Life Sciences & Biomedicine; MCF-7 Cells; Models, Molecular; molecular docking; Molecular Structure; Pharmacology & Pharmacy; Quinazolines - chemical synthesis; Quinazolines - chemistry; Quinazolines - pharmacology; Receptor, Epidermal Growth Factor - antagonists & inhibitors; Science & Technology; Structure-Activity Relationship; TYROSINE KINASE INHIBITORS; IRREVERSIBLE INHIBITORS; 4-anilinoquinazolines; molecular docking; epidermal growth factor receptor (EGFR); CANCER; antitumor agents
• ISSN: 1860-7179; 1860-7187
• DOI: 10.1002/cmdc.201300120

Strike a pose! A series of 4‐anilinoquinazolines were designed, synthesized and evaluated in vitro against lung and breast cancer cell lines. Several compounds were found to be endowed with cytotoxicity in the low micromolar range. Molecular docking suggests that these compounds bind to EGFR in a similar manner to known EGFR inhibitors.