Yu Congtao, Gao Chuanzhu, Bai Linkui, Liu Qinghua, Zhang Zhuxin, Zhang Yingjie, Yang Bo, Li Chunli, Dong Peng, Sun Xiaojun, Qian Yunxu
Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China.
Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China.
Bioorg Med Chem Lett. 2017 Feb 15;27(4):963-966. doi: 10.1016/j.bmcl.2016.12.084. Epub 2016 Dec 31.
Six dinuclear platinum(II) complexes with a chiral tetradentate ligand, (1R,1'R,2R,2'R)-N,N-(1,4-phenylenebis(methylene))dicyclohexane-1,2-diamine, have been designed, synthesized and characterized. In vitro cytotoxicity evaluation of these metal complexes against human A549, HCT-116, MCF-7 and HepG-2 cell lines have been carried out. All compounds showed antitumor activity to HepG-2, HCT-116 and A549. Particularly, compounds A1 and A2 exhibited significant better activity than other four compounds and A2 even showed comparable cytotoxicity to cisplatin against HepG-2 cell line.
设计、合成并表征了六种带有手性四齿配体（1R,1'R,2R,2'R）-N,N-（1,4-亚苯基双（亚甲基））二环己烷-1,2-二胺的双核铂（II）配合物。对这些金属配合物针对人A549、HCT-116、MCF-7和HepG-2细胞系进行了体外细胞毒性评估。所有化合物对HepG-2、HCT-116和A549均表现出抗肿瘤活性。特别地，化合物A1和A2表现出比其他四种化合物显著更好的活性，并且A2对HepG-2细胞系甚至表现出与顺铂相当的细胞毒性。
