Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research, Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, China.
Arch Pharm (Weinheim). 2013 Apr;346(4):308-13. doi: 10.1002/ardp.201200288. Epub 2013 Feb 28.
Five novel dinuclear platinum(II) complexes with a new chiral ligand, 3-(2-amino-cyclohexylamino)-propionic acid (HP), were designed, prepared and spectrally characterized. The in vitro cytotoxicities of these compounds were evaluated against the HepG-2, MCF-7, A549, and HCT-116 cell lines. The results indicated that all compounds showed cytotoxicity towards the HepG-2 cell line. Particularly, complex X5, which has SO 4₂₋ as a bridge, exhibited better cytotoxicity than carboplatin or oxaliplatin against all selected cell lines. Moreover, double dyeing flow cytometric resection indicated that the target compounds inhibited tumor cell growth by inducing apoptosis.
设计、合成并光谱表征了 5 种新型双核铂（II）配合物，该配合物以新型手性配体 3-(2-氨基环己基氨基）-丙酸（HP）为配体。测试了这些化合物对 HepG-2、MCF-7、A549 和 HCT-116 细胞系的体外细胞毒性。结果表明，所有化合物对 HepG-2 细胞系均具有细胞毒性。特别是具有 SO₄₂₋桥的化合物 X5 对所有选定的细胞系的细胞毒性优于顺铂或奥沙利铂。此外，双染流式细胞术分析表明，这些靶化合物通过诱导细胞凋亡抑制肿瘤细胞生长。
