INSERM UMR U866 "Lipides/Nutrition/Cancer", Université de Bourgogne, UFR Médecine, 7 bd Jeanne d'Arc, BP 89700, 21079 Dijon Cedex, France.
Eur J Med Chem. 2013 Nov;69:719-27. doi: 10.1016/j.ejmech.2013.09.037. Epub 2013 Sep 26.
A novel family of cisplatin-type complexes tethered to dibenzo[c,h][1,6]naphthyridin-6-one topoisomerase inhibitor via a polymethylene chain and their nonplatinated counterparts were prepared. Their potential cytotoxicity was assessed in three human colorectal cancer cell lines HCT 116, SW480 and HT-29 and compared to the reference molecules cisplatin and oxaliplatin. Platinated compounds were poorly active whilst nonplatinated dibenzo[c,h][1,6]naphthyridin-6-one moieties exhibited higher cytotoxic properties than cisplatin and oxaliplatin whatever the length of the polymethylene chain; molecules containing the tri- and hexamethylene chain length were the most cytotoxic.
通过亚甲基链将一类新型顺铂型配合物连接到苯并[c,h][1,6]萘啶-6-酮拓扑异构酶抑制剂上，并制备了它们的非铂类似物。在三种人结肠直肠癌细胞系 HCT 116、SW480 和 HT-29 中评估了它们的潜在细胞毒性，并与参考分子顺铂和奥沙利铂进行了比较。铂化化合物活性较差，而无论亚甲基链的长度如何，非铂化苯并[c,h][1,6]萘啶-6-酮部分都表现出比顺铂和奥沙利铂更高的细胞毒性；含有三甲基和六亚甲基链长的分子具有最强的细胞毒性。
