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

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• 作者：Song Yang ; Zhi Li ; Linhong Jin ; Baoan Song ; Gang Liu ; Jiang Chen ; Zhuo Chen ; Deyu Hu ; Wei Xue ; Ruiqing Xu
• 关键词：Quinazoline ; Thioether ; Synthesis ; Anti-cancer activity ; Against ERK phosphorylation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 April 2007
• 卷：17
• 期：8
• 页码：2193-2196
• 文件大小：275 K

摘要

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.