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