Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Design and Synthesis of Novel Epidermal Growth Factor Receptor Kinase Inhibitors

  • Ha, Jae-Du (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Kang, Seung-Kyu (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Kim, Kun-Do (Department of Microbiology, Pukyong National University) ;
  • Choi, Joong-Kwon (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Kong, Jae-Yang (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Ahn, Chang-H. (Rexahn Corporation, 9620 Medical Center)
  • Published : 2005.06.20
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Abstract

Investigation of structure-activity relationships of novel quinazolines has identified 7,8-dihydro-[1,4]dioxino-[2,3-g]quinazolines as a potent inhibitor of EGFR. These compounds have a benzodioxane framwork, which was prepared by regioselective O-alkylation of ethyl 3,4-dihydroxy benzoate by epoxide ring opening. Compounds 3f and 3k were more potent than ZD-1839 in EGF enzyme and EGFR autophosporylation inhibition assays.

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References

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