Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors

  • Bioorg Med Chem Lett. 2012 Oct 1;22(19):6301-5. doi: 10.1016/j.bmcl.2012.06.067.
Shaojing Hu  1 ,  Guojian Xie ,  Don X Zhang ,  Charles Davis ,  Wei Long ,  Yunyan Hu ,  Fei Wang ,  Xinshan Kang ,  Fenlai Tan ,  Lieming Ding ,  Yinxiang Wang
Affiliations
  • 1. Zhejiang Betapharma, 589 Hongfong Rd., YuhangDistrict, Zhejiang 311100, PR China. [email protected]
PMID: 22959248 DOI: 10.1016/j.bmcl.2012.06.067
Abstract

Crown ether fused anilinoquinazoline analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities in an in vitro EGFR kinase assay and an EGFR-mediated intracellular tyrosine phosphorylation assay. The synthesis and preliminary biological, physical, and pharmacokinetic evaluation of these fused quinazoline compounds is reported.