Epidermal growth factor receptor tyrosine kinase: Structure-activity relationships and antitumour activity of novel quinazolines

Article abstract of DOI:10.1016/S0960-894X(97)10059-2

Investigation of structure-activity relationships of novel quinazolines has identified 4-(4-isoquinolylamino)-quinazoline and a 4-(trans-2-phenylcyclopropylamino)-quinazoline as potent inhibitors of EGF-receptor tyrosine kinase in vitro. Further modificatons of the latter compound have identified a derivative which shows anti-tumour activity against a tumour xenograft model when dosed orally once per day.