对氯苄基锡酰腙配合物的合成、抗肿瘤活性及其与DNA相互作用

用二对氯苄基二氯化锡分别与对甲基苯甲酰肼缩苯甲酰甲酸及苯甲酰肼缩苯甲酰甲酸反应,合成了2个对氯苄基锡配合物(C1、C2),通过元素分析、IR、1 H NMR、13C NMR、119Sn NMR、HRMS以及X射线单晶衍射等表征了配合物结构。测试了配合物C1、C2的热稳定性以及配合物对癌细胞NCI?H460、HepG2、MCF7的体外抑制活性,发现配合物C2对癌细胞NCI?H460、HepG2、MCF7等均表现出良好的抑制作用。利用紫外吸收光谱、荧光猝灭光谱以及粘度法研究了配合物C2与ct?DNA之间的相互作用,结果表明配合物C2以插入模式与DNA结合。

Syntheses, Antitumor Activity and DNA Interaction of p-Chlorine-Benzyltin Complexes Based on Acylhydrazone Ligand

Two p-chlorobenzyltin complexes have been synthesized via the reaction of p-methyl benzoyl hydrazidebenzoyl formic acid or benzoyl hydrazide-benzoyl formic acid with di-p-chlorobenzyltin dichloride. The complexes C1 and C2 have been characterized by IR, ¹H NMR, ¹³C NMR, ¹¹⁹Sn NMR spectra, elemental analysis and HRMS, and the crystal structures have been determined by X-ray diffraction. The thermogravimetric of the complexes C1 and C2 were analyzed, and in vitro antitumor activities of both complexes were evaluated by MTT (3-(4,5-dimethyl-thiazole-2)-2,5-diphenyltetrazolium bromide) against three human cancer cell lines (NCI-H460, HepG2 and MCF7). It was found that complex C2 showed a good inhibitory effect on cancer cells NCI-H460, HepG2, MCF7. The interaction of complex C2 with DNA was investigated using electronic absorption spectroscopy, fluorescence quench, and viscosity measurement. It was found that the complex could bind to DNA through an intercalation mode.