2. Academic Validation
  3. Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors

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

  • Bioorg Med Chem Lett. 2016 Mar 15;26(6):1571-1575. doi: 10.1016/j.bmcl.2016.02.009.
Xuemei Qin 1,  Yongjuan Lv 1,  Peng Liu 2,  Zhipeng Li 1,  Liming Hu 3,  Chengchu Zeng 1,  Leifu Yang 4
Affiliations

Affiliations

  • 1 College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China.
  • 2 Guangzhou Institute of Biomedicine and Health, Chinese Academy of Science, Guangzhou 510530, China.
  • 3 College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China. Electronic address: huliming@bjut.edu.cn.
  • 4 Beijing Dalitai Pharmaceutical Technology Co. Ltd, Beijing 100176, China.
PMID: 26879314 DOI: 10.1016/j.bmcl.2016.02.009
Abstract

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 EGFR(wt) kinase (IC50<1 μM). Compound a8 demonstrated the most potent inhibitory activity toward EGFR(wt) (IC50=53.1 nM). Compound a7 and a8 showed excellent inhibitory activities against mutant EGFR(T790M/L858R) and strong antiproliferative activity against H358 and A549 cell lines. Finally, molecular docking studies were performed to predict the possible binding mode of the target compounds. It is believed that this work would be very useful for designing a new series of tyrosine kinase inhibitors targeting EGFR.

Keywords

Anti-cancer; EGFR inhibitors; Molecular docking; NSCLC; Quinazoline.

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