Synthesis of novel benzoxanthone analogues as non-Camptothecin topoisomerase I inhibitors
作者:Pengfei Cheng、Lingjian Zhu、Wei Guo、Wenfeng Liu、Jianzhong Yao、Guoqiang Dong、Yongqiang Zhang、Chunlin Zhuang、Chunquan Sheng、Zhenyuan Miao、Wannian Zhang
DOI:10.3109/14756366.2011.595712
日期:2012.6.1
Structure modification of the side chain of the lead compound benzoxanthone provided a series of benzoxanthone analogues and 12 of them were first reported. The results showed that most of these compounds had moderate cytotoxicity against tumour cells with the 50% inhibition concentration in the micromolar range. Furthermore, benzoxanthone derivatives 5, 6c, 7a and 7e, showed potent topoisomerase I (Topo
铅化合物苯并an吨酮侧链的结构修饰提供了一系列苯并an吨酮类似物,其中首次报道了其中的12个。结果表明,这些化合物中的大多数对肿瘤细胞具有中等的细胞毒性,在微摩尔范围内的抑制浓度为50%。此外,苯并an吨酮衍生物5、6c,7a和7e表现出强力的拓扑异构酶I(Topo I)抑制作用,结果表明某些化合物具有发展为非喜树碱(CPT)拓扑异构酶I抑制剂的潜力。