Design and Synthesis of Novel Epidermal Growth Factor Receptor Kinase Inhibitors

Bulletin of the Korean chemical society

Jae Yang Kong¹  Joong-Kwon Choi¹  Jae Du Ha¹  Kun-Do Kim¹  Seung Kyu Kang¹  Chang H. Ahn¹ 

关键词: Cancer;    EGFR;    Tyrosine kinase;    Quinazoline;    Autophosphorylation assay;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown