N-((2-甲基-4(3H)-喹唑啉酮-6-基)甲基)二硫代氨基甲酸盐的合成及细胞毒性活性。
Synthesis and cytotoxic activity of N-((2-methyl-4(3H)-quinazolinon-6-yl)methyl)dithiocarbamates.
机构信息
Department of Chemistry, Capital Normal University, Beijing 100048, PR China.
出版信息
Eur J Med Chem. 2010 Sep;45(9):3850-7. doi: 10.1016/j.ejmech.2010.05.038. Epub 2010 May 25.
A series of N-((2-methyl-4(3H)-quinazolinon-6-yl)methyl)dithiocarbamates 5a-w were synthesized and evaluated for their cytotoxic activity against five human cancer cell lines. We found that compound 5k inhibited proliferation of A549, MCF-7, HeLa, HT29 and HCT-116 cells with IC(50) values of 5.44, 7.15, 12.16, 10.35 and 11.44 microM, respectively. Compound 5i was the most potent with an IC(50) value of 3.65 microM against proliferation of MCF-7 cells, while 5n was the most potent with an IC(50) value of 5.09 microM against proliferation of A549 cells. Cell cycle analysis showed that both 5i and 5k arrested A549 cells at S and G2/M phases, suggesting that these compounds act through mechanisms different from 5-fluorouracil, which arrests cells at S phase only.
一系列 N-((2-甲基-4(3H)-喹唑啉-6-基)甲基)二硫代氨基甲酸盐 5a-w 被合成并评估了它们对五种人癌细胞系的细胞毒性活性。我们发现化合物 5k 对 A549、MCF-7、HeLa、HT29 和 HCT-116 细胞的增殖具有抑制作用，IC50 值分别为 5.44、7.15、12.16、10.35 和 11.44 microM。化合物 5i 对 MCF-7 细胞的增殖具有最强的抑制活性，IC50 值为 3.65 microM，而 5n 对 A549 细胞的增殖具有最强的抑制活性，IC50 值为 5.09 microM。细胞周期分析表明，化合物 5i 和 5k 均可将 A549 细胞阻滞在 S 和 G2/M 期，表明这些化合物的作用机制与仅在 S 期阻滞细胞的 5-氟尿嘧啶不同。
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