2. Academic Validation
  3. Design, synthesis and biological evaluation of novel 3,4-dihydro-2H-[1,4]oxazino [2,3-f]quinazolin derivatives as EGFR-TKIs

Design, synthesis and biological evaluation of novel 3,4-dihydro-2H-[1,4]oxazino [2,3-f]quinazolin derivatives as EGFR-TKIs

  • Bioorg Med Chem Lett. 2023 Jan 15:80:129104. doi: 10.1016/j.bmcl.2022.129104.
Xuemei Qin 1,  Peng Liu 2,  Yihai Li 3,  Liming Hu 4,  Yexin Liao 5,  Tingting Cao 4,  Lifang Yang 6
Affiliations

Affiliations

  • 1 Guangxi Key Laboratory of Polysaccharide Materials and Modifications, School of Marine Sciences and Biotechnology, Guangxi Minzu University, Nanning 530008, China; Key Laboratory of Protection and Utilization of Marine Resources, Guangxi Minzu University, Nanning 530008, China. Electronic address: qxmei313@126.com.
  • 2 Guangzhou Institute of Biomedicine and Health, Chinese Academy of Science, Guangzhou 510530, China.
  • 3 Guangxi Key Laboratory of Polysaccharide Materials and Modifications, School of Marine Sciences and Biotechnology, Guangxi Minzu University, Nanning 530008, China.
  • 4 College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China.
  • 5 School of Chemistry and Chemical Engineering, Guangxi Minzu University, Guangxi Nanning 530008, China.
  • 6 School of Chemistry and Chemical Engineering, Guangxi Minzu University, Guangxi Nanning 530008, China. Electronic address: yanglf1990@163.com.
PMID: 36509365 DOI: 10.1016/j.bmcl.2022.129104
Abstract

Starting with our previously reported work, a novel series of 3,4-dihydro-2H-[1,4]oxazino[2,3-f]quinazolin-derivatives were designed, synthesized and evaluated as potent EGFR tyrosine kinase inhibitors. All of the compounds showed significant inhibitory activities against EGFRwt kinase (IC50 ≤ 937.7 nM). Among them, compound 7j demonstrated the most potent inhibitory activity toward EGFRwt tyrosine kinase with IC50 value of 25.69 nM and showed good antiproliferative activities against NCI-H1563 and H1975 cells. The median cytotoxic concentration (CC50) showed that most of the tested compounds displayed almost no cytotoxicity in vitro against 16HBE cells. In view of the reported compounds activity, the structure deserves further optimization as Cancer treatment agents.

Keywords

EGFR inhibitors; NSCLC; Quinazolin derivatives; Tyrosine kinases.

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