氮杂Brazilin-咪唑盐杂合物的设计、合成及细胞毒活性研究

Design, Synthesis and Cytotoxic Activity of Novel Hybrid Compounds between Aza-brazilin and Imidazolium

从3,4-二甲氧基苯丙酸出发合成了一系列新型的氮杂Brazilin-咪唑盐杂合物,其结构经1H NMR,13C NMR,HR-ESI-MS以及X射线单晶衍射确定.对合成的新化合物进行了体外抗肿瘤活性筛选,发现3-(萘-2-甲基)-1-(2-氧代-2-(4,9,10-三甲氧基-6,6a,7,11b-四氢茚并[2,1-c]喹啉-5-基)乙基)-2-甲基苯并咪唑溴盐(26)具有较好的细胞毒活性,对4种肿瘤细胞株的活性均优于顺铂,特别是对HL-60、MCF-7和SW-480表现出较好的和选择性的细胞毒活性.

A series of novel hybrid compounds between aza-brazilin and imidazole have been prepared from 3-（3,4-dimethoxyphenyl）propanoic acid. Their structures were confirmed by 1H NMR, 13 C NMR, HR-ESI-MS and X-ray crystallographic analysis. These compounds have been evaluated in vitro against a panel of human tumor cell lines. 2-Methyl-3-（naphthalen-2-ylmethyl）-1-（2-oxo-2-（4,9,10-trimethoxy-6,6a,7,11b-tetrahydro-5H-indeno[2,1-c]quinolin-5-yl）ethyl）-1H-benzo[d]imidazol-3-ium bromide（26） was found to be the most potent derivative against four strains human tumor lines and more active than cisplatin, and exhibited the most potent cytotoxic activities selectively against HL-60, MCF-7 and SW-480.