Design, synthesis and in vitro biological evaluation of quinazolinone derivatives as EGFR inhibitors for antitumor treatment

• Published in: Journal of enzyme inhibition and medicinal chemistry Vol. 35; no. 1; pp. 555 - 564
• Main Authors: Le, Yi, Gan, Yiyuan, Fu, Yihong, Liu, Jiamin, Li, Wen, Zou, Xue, Zhou, Zhixu, Wang, Zhenchao, Ouyang, Guiping, Yan, Longjia
• Format: Journal Article
• Language: English
• Published: ABINGDON Taylor & Francis 01.01.2020; Taylor & Francis Ltd; Taylor & Francis Group
• Subjects: A549 Cells; Amino acids; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; antitumor; Antitumor activity; Apoptosis; Apoptosis - drug effects; Biochemistry & Molecular Biology; Cell cycle; Cell Cycle - drug effects; Cell Proliferation - drug effects; Chemistry, Medicinal; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; EGFR; Epidermal growth factor; Epidermal growth factor receptors; ErbB Receptors - antagonists & inhibitors; ErbB Receptors - metabolism; Humans; Hydrogen bonding; Life Sciences & Biomedicine; Models, Molecular; molecular docking; Molecular Structure; Pharmacology & Pharmacy; Protein Kinase Inhibitors - chemical synthesis; Protein Kinase Inhibitors - chemistry; Protein Kinase Inhibitors - pharmacology; Protein-tyrosine kinase receptors; Quinazolinone; Quinazolinones - chemical synthesis; Quinazolinones - chemistry; Quinazolinones - pharmacology; Rapid Communication; Science & Technology; Short Communication; Structure-Activity Relationship; Tumor cell lines; tyrosine kinase inhibitor; molecular docking; antitumor; KINASE; RESISTANCE; BEARING; Quinazolinone; tyrosine kinase inhibitor; DUAL INHIBITORS; EGFR

In this paper, a series of novel 3-methyl-quinazolinone derivatives was designed, synthesised and evaluated for antitumor activity in vitro on wild type epidermal growth factor receptor tyrosine kinase (EGFR wt -TK) and three human cancer cell lines including A549, PC-3, and SMMC-7721. The results d...