الفهرس | Only 14 pages are availabe for public view |
Abstract Cancer is a disease where some of normal cells were modified to abnormal ones with a very good perfusion of blood supply, this modification include a lot of genetic changes. Quinazolines and hence quinazolinones have attracted our attention and interest due to their wide range of pharmacological activity specially their anticancer one. The present study deals with the synthesis of new quinazolinone derivatives based on the key intermediate 3-amino-2-(4- bromophenoxymethyl)-6-iodo-3H-quinazolin-4-one (IV) via reaction with the appropriate aldehyde, acetic anhydride, isatin or choloroacetyl chloride to produce Va-c, VIa-c, VII, VIII and IX respectively. Further reaction of the choloroacetamido IX with the appropriate secondary amine or 4-oxo-6- un/substituted phenyl-2-thioxopyrimidine-5-carbonitrile gave Xa-c and XIIa-c respectively. Fifteen newly compounds were synthesized and tested for their in vitro: anticancer activity against MCF-7 (breast), A-549 (lung), HCT-116 (colon) cancer cell lines in addition to normal fibroblasts WI-38. Eight compounds showing promising anticancer activity were further screened for their EGFR inhibitory activity compared to geftinib |