Design and Synthesis of Novel Epidermal Growth Factor Receptor Kinase Inhibitors

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 epoxid...

Full description

Saved in:
Bibliographic Details
Published in:Bulletin of the Korean Chemical Society 2005, 26(6), , pp.959-965
Main Authors: Ha, Jae-Du, Kang, Seung-Kyu, Kim, Kun-Do, Choi, Joong-Kwon, Kong, Jae-Yang, Ahn, Chang-H
Format: Article
Language:Korean
Subjects:
화학
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0253-2964
1229-5949