Synthesis and in vitro antitumor activities of xanthone derivatives containing 1,4-disubstituted-1,2,3-triazole moiety
作者:Yan Zou、Qingjie Zhao、Honggang Hu、Lina Hu、Shichong Yu、Mingjuan Xu、Qiuye Wu
DOI:10.1007/s12272-012-1206-4
日期:2012.12
To explore the more active antitumor compounds, two series of new xanthones, containing 1,4-disubstituted-1,2,3-triazole moiety were designed and synthesized. Eaton’s Reagent and “click reaction” were used in the synthesis. Most of the title compounds showed good inhibitory activity against the hepatoma carcinoma cell line (Bel-7402) and human cervical carcinoma cell line (HeLa) in vitro. Compounds
为了探索更具活性的抗肿瘤化合物,设计并合成了两个系列的含有 1,4-二取代-1,2,3-三唑部分的新型氧杂蒽酮。合成中使用了伊顿试剂和“点击反应”。大多数标题化合物在体外对肝癌细胞系 (Bel-7402) 和人宫颈癌细胞系 (HeLa) 显示出良好的抑制活性。化合物 10a、10e、10f、11r 和 11t 具有强活性,IC50 值范围为 2.2 ± 0.17 至 7.1 ± 0.27 ∝M,相当于阿霉素。