Synthesis and in vitro antitumor activity of substituted quinazoline and quinoxaline derivatives: Search for anticancer agent

► Synthesis of some 2-furano-4(3H)-quinazolinones, diamides (open ring quinazolines), quinoxalines and their biological evaluation as antitumor agents using National Cancer Institute (NCI) disease oriented antitumor screen protocol investigated. ► Seventeen compounds were granted NSC code. ► 3-(2-chloro benzylideneamine)-2-(furan-2-yl) quinazoline-4(3h)-one 21 (NSC D-753439/1) was found to be the most active candidate of the series at five dose level. ► Rational approach and QSAR techniques enabled the understanding of the pharmacophoric requirement for quinazoline, diamides (open ring quinazolines) and quinoxaline derivatives.