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Updated: Sep 27, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
7-Substituted-[1,4]dioxano[2,3-g]quinazolines as inhibitors of epidermal growth factor receptor kinase
Jae Yeol Lee1, Yong Kyu Park, Seon Hee Seo
1Medicinal Chemistry Research Center, Korea Institute of Science & Technology, P.O. Box 131, Cheongryang, Seoul 130-650, Korea.
Abstract:
With the aim of developing inhibitors of EGFR tyrosine kinase, the 7-methoxymethyl-[1,4]dioxano[2,3-g]quinazolines (3a-b) and 7-mono- or di-alkylaminomethyl-[1,4]dioxano[2,3-g]quinazolines (4a-i) were prepared and evaluated for the inhibition of EGFR tyrosine kinase and the growth inhibition of human tumor cell lines. Among them, compounds 4d and 4h showed potencies against both EGFR tyrosine and the A431 cell line similar to that of PD153035 with greater aqueous solubilities of their HCl salts.
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