EPIDERMAL GROWTH-FACTOR RECEPTOR TYROSINE KINASE - STRUCTURE-ACTIVITY-RELATIONSHIPS AND ANTITUMOR-ACTIVITY OF NOVEL QUINAZOLINES

Authors
GIBSON KH GRUNDY W GODFREY AA WOODBURN JR ASHTON SE CURRY BJ SCARLETT L BARKER AJ BROWN DS
Citation
Kh. Gibson et al., EPIDERMAL GROWTH-FACTOR RECEPTOR TYROSINE KINASE - STRUCTURE-ACTIVITY-RELATIONSHIPS AND ANTITUMOR-ACTIVITY OF NOVEL QUINAZOLINES, Bioorganic & medicinal chemistry letters, 7(21), 1997, pp. 2723-2728
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
21
Year of publication
1997
Pages
2723 - 2728
Database
ISI
SICI code
0960-894X(1997)7:21<2723:EGRTK->2.0.ZU;2-Y
Abstract
Investigation of structure-activity relationships of novel quinazoline s has identified a 4-(4-iso-quinolylamino)-quinazoline and a 4-(trans- 2-phenylcyclopropylamino)-quinazoline as potent inhibitors of EGF-rece ptor tyrosine kinase in vitro. Further modifications of the latter com pound have identified a derivative which shows anti-tumour activity ag ainst a tumour xenograft model when dosed orally once per day. (C) 199 7 Elsevier Science Ltd.