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7-Substituted-[1, 4]dioxano[2, 3-g]quinazolines as Inhibitors of Epidermal Growth Factor Receptor Kinase

✍ Scribed by Jae Yeol Lee; Yong Kyu Park; Seon Hee Seo; Beom-Seok Yang; Hokoon Park; Yong Sup Lee

Publisher: John Wiley and Sons
Year: 2002
Tongue: English
Weight: 123 KB
Volume: 335
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.200290003

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✦ Synopsis

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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