Synthesis and bioactivity of 4-alkyl(aryl)thioquinazoline derivatives

Abstract

Some S'-substituted 4-alkyl(aryl)thioquinazoline derivatives were synthesized through thioetherification reaction of 4-chloroquinazolines 2 and thiol compounds 1 refluxed in acetone in the presence of K(2)CO(3). Their structures were verified by elemental analysis, IR, (1)H NMR, and (13)C NMR. The compounds were evaluated for their anti-proliferative activities against some cancer cells in vitro by MTT method. Among them, 3c, 3a, 3d, 3f, and 3l were highly effective against PC3 cells and 3a-3m showed weak activities against Bcap37 and BGC823 cells. The IC(50) value of 3c, 3a, 3d, 3f, and3l against PC3 cell was 1.8, 5.6, 8.1, 8.7, and 8.9 microM, respectively.