title: 7-Substituted-[1,4]dioxano[2,3-g]quinazolines as inhibitors of epidermal growth factor receptor kinase.
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.
authors.affiliation: Medicinal Chemistry Research Center, Korea Institute of Science & Technology, P.O. Box 131, Cheongryang, Seoul 130-650, Korea.
authors.forename: Jae Yeol
authors.initials: JY
authors.lastname: Lee
authors.forename: Yong Kyu
authors.initials: YK
authors.lastname: Park
authors.forename: Seon Hee
authors.initials: SH
authors.lastname: Seo
authors.forename: Beom-Seok
authors.initials: BS
authors.lastname: Yang
authors.forename: Hokoon
authors.initials: H
authors.lastname: Park
authors.forename: Yong Sup
authors.initials: YS
authors.lastname: Lee
mesh_terms: D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000502:physiology; D006801:Humans; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D011799:Quinazolines; D066246:ErbB Receptors