State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Chemical Engineering of Guangxi Normal University, Guilin 541004, PR China.
Eur J Med Chem. 2013 Apr;62:51-8. doi: 10.1016/j.ejmech.2012.12.030. Epub 2012 Dec 23.
Three tin(IV) complexes [Sn(ClQ)2Cl2] (1), [Sn(BrQ)2Cl2] (2) and [Sn(ClIQ)2Cl2] (3) were prepared (H-ClQ = 5,7-dichloro-8-hydroxylquinoline, H-BrQ = 5,7-dibromo-8-hydroxylquinoline, H-ClIQ = 5-chloro-7-iodo-8-hydroxylquinoline) and their in vitro cytotoxicities against BEL7404, SKOV-3, NCI-H460, HL-7702 cell lines were evaluated. The complexes showed high anti-proliferative activity toward the tested cell lines with IC50 values ranging from 20 nM to 5.11 μM. Compared with 5,7-dihalo-8-quinolinol, most complexes exhibited significantly enhanced cytotoxicity (except 2 against SKOV-3 and NCI-H460). They also displayed some selective cytotoxicity favoring the tested tumor cells over the normal human liver HL-7702 cells. Compared with their quinolinol ligands, complexes 1-3 bind more strongly with DNA. Intercalation is the most probable binding mode for both the complexes and their quinolinol ligands.
合成了三种锡(IV)配合物[Sn(ClQ)2Cl2]（1）、[Sn(BrQ)2Cl2]（2）和[Sn(ClIQ)2Cl2]（3）（H-ClQ = 5,7-二氯-8-羟基喹啉，H-BrQ = 5,7-二溴-8-羟基喹啉，H-ClIQ = 5-氯-7-碘-8-羟基喹啉），并评价了它们对 BEL7404、SKOV-3、NCI-H460 和 HL-7702 细胞系的体外细胞毒性。这些配合物对测试的细胞系表现出很高的抗增殖活性，IC50 值范围为 20 nM 至 5.11 μM。与 5,7-二卤代-8-喹啉醇相比，大多数配合物表现出显著增强的细胞毒性（除 2 对 SKOV-3 和 NCI-H460 外）。它们还表现出一些选择性细胞毒性，有利于测试的肿瘤细胞而不是正常的人肝 HL-7702 细胞。与它们的喹啉醇配体相比，配合物 1-3 与 DNA 的结合更强。对于两种配合物及其喹啉醇配体，插入是最可能的结合模式。
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