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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 26, Number 6
BKCSDE 26(6)
June 20, 2005 

Design and Synthesis of Novel Epidermal Growth Factor Receptor Kinase Inhibitors
Jae Du Ha*, Seung Kyu Kang, Kun-Do Kim, Joong-Kwon Choi, Jae Yang Kong, Chang H. Ahn
Cancer, EGFR, Tyrosine kinase, Quinazoline, Autophosphorylation assay
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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