A novel compound, Cou-platin, composed of 7-hydroxycoumarin and a platinum(IV) moiety derived from cisplatin was designed and synthesized. Significantly, Cou-platin exhibited more potent in vitro antitumor activity against all tested cancer cell lines than that of cisplatin, which was mainly attributed to the liberation of cisplatin and 7-hydroxycoumarin upon reduction with a biomolecular agent. Besides, cellular accumulation of Cou-platin was dramatically increased among several cancer cells in contrast to cisplatin. Flow cytometry study revealed that Cou-platin arrested cell cycle at G2 phase and induced cell apoptosis. Western blots results indicated that it not only activated cell apoptosis pathway, but also inhibited extracellular regulated protein kinases/mitogen-activated protein kinase pathway. In vivo tests showed that Cou-platin, at equimolar dose to cisplatin, could inhibit tumor growth in nude mouse HCT116 tumor xenograft models almost as cisplatin and oxaliplatin, but with less toxicity.

设计合成了由7-羟基香豆素和顺铂衍生的铂（IV）部分组成的新型化合物库铂。值得注意的是，Cou-Platin对所有测试的癌细胞系均表现出比顺铂更强的体外抗肿瘤活性，这主要归因于生物分子试剂还原后顺铂和7-羟基香豆素的释放。此外，与顺铂相反，在一些癌细胞中，Cou-Platin的细胞积累显着增加。流式细胞仪研究表明，Cou-Platinin在G2期阻止了细胞周期并诱导了细胞凋亡。蛋白质印迹结果表明，它不仅激活细胞凋亡途径，而且抑制细胞外调节的蛋白激酶/丝裂原激活的蛋白激酶途径。体内测试显示，Cou-Platin，