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7‐Substituted‐[1, 4]dioxano[2, 3‐ g ]quinazolines as Inhibitors of Epidermal Growth Factor Receptor Kinase
Author(s) -
Lee Jae Yeol,
Park Yong Kyu,
Seo Seon Hee,
Yang BeomSeok,
Park Hokoon,
Lee Yong Sup
Publication year - 2002
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200290003
Subject(s) - tyrosine kinase , chemistry , epidermal growth factor receptor , a431 cells , epidermal growth factor , platelet derived growth factor receptor , cell culture , receptor tyrosine kinase , kinase , biochemistry , pharmacology , receptor , cell , growth factor , biology , cell cycle , genetics , molecular medicine
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.