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Updated: Jul 16, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis and bioactivity of 4-alkyl(aryl)thioquinazoline derivatives
Song Yang1, Zhi Li, Linhong Jin
1Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China.
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.
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