2-羰基-2-苯基乙酸对羟基苯甲酰腙二丁基锡配合物的合成、晶体结构及生物活性研究

Synthesis,Crystal Structure and Biological Activity of the 2-Oxo-2-Phenylacetic Acid Aroyl Hydrazine Dibutyltin Complex

2-羰基-2-苯基乙酸对羟基苯甲酰腙和二丁基氧化锡反应,合成了一个2-羰基-2-苯基乙酸对羟基苯甲酰腙二丁基锡配合物,通过元素分析、IR、单晶X-射线衍射、TGA、1 H NMR和13 C NMR等表征了配合物分子结构和性质。采用MTT方法,研究了该二丁基锡配合物对癌细胞MCF7、Hela、NCI-H460、HepG2、Colo205的体外抗癌活性以及对正常人体肝细胞(HL7702),人体胚肾细胞(HEK293)的体外抑制活性;用荧光光谱法初步研究了配合物与小牛胸腺DNA的相互作用。结果表明:该酰腙类二丁基锡配合物(1)对5种癌细胞都有明显的抑制作用;与CT DNA的作用类型为插入结合。

The 2-oxo-2-phenylacetic acid aroyl hydrazine dibutyltin complex （1） has been synthesized via the reaction of the 2- oxo-2-phenylacetic acid aroyl hydrazine with the dibutyhin oxide. The complex （1） has been characterized by FT-IR,JH NMR, 13 C NMR spectra, elemental analysis, thermal analysis and X-ray diffraction.The anticancer activity of the complex （ 1 ） a- gainst five species of cancer cell which are Hela, MCF7, HepG2, Colo205, NCI-H460 and Human normal cell line HEK293, HL7702 were tested respectively. The interaction between complex and Calf Thymus DNA were studied by EB fluorescent probe, the result shows that the interaction of the complex with Calf Thymus DNA were intercalation and electrostatic attraction.