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

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 K2CO3. Their structures were verified by elemental analysis, IR, 1H NMR, and 13C 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 IC50 value of 3c, 3a, 3d, 3f, and3l against PC3 cell was 1.8, 5.6, 8.1, 8.7, and 8.9 μM, respectively.

A series of S′-substituted 4-alkyl(aryl)thioquinazoline derivatives were synthesized through thioetherification of 4-chloroquinazolines and thiol compounds refluxed in acetone in the presence of K2CO3. And their inhibitory activities against cancer cells were bioassayed.Figure optionsDownload as PowerPoint slide