含分子内配位作用的环状铋(Ⅲ)化合物抑制人乳腺癌MCF-7细胞增殖的初步研究

Study on Anti-proliferative Activity Against Human Breast Adenocarcinoma Cells MCF-7 of Heterocyclic Organobismuth(Ⅲ)Complexes with Intramolecular E→Bi Coordinate Bond

利用CCK-8法考察了5种具有分子内E→Bi配位作用(E=O,N,S)的环状铋(Ⅲ)化合物对MCF-7人乳腺癌细胞的体外抑制活性。研究结果表明,这些铋化合物对MCF-7肿瘤细胞均有一定程度的抗增殖作用,且该系列铋(Ⅲ)化合物对肿瘤细胞的生长抑制作用明显优于常用的抗肿瘤药物顺铂。构-效关系研究结果表明,通过改变配位原子的类型及配体骨架的空间位阻能够实现对该类铋(Ⅲ)化合物抗肿瘤活性的调控。

The in vitro antitumor activity of five heterocyclic organobismuth(Ⅲ)complexes containing intramolecular E→Bi coordinate bond(E=O,N,S)against human breast adenocarcinoma cells(MCF-7)has been investigated in this work using the CCK-8 method.Our results show that the antitumor performance against MCF-7 cell lines of these organobismuth(Ⅲ)compounds was more potent than that of the commonly available cisplatin.And the results of our structure-activity relationship(SAR)study demonstrate that the pharmaceutical effect of these heterocyclic organobismuth(Ⅲ)compounds could be precisely regulated by adjusting the type of the coordination atom and the steric hindrance of ligand.