4-叔丁基-5-(12,4,-三唑-1-基)-2-苄亚氨基噻唑的体外抗癌活性研究  

Anticancer activity of(E)-N-benzylidene-4-tert-butyl-5-(1,2,4-triazol-1-yl)thiazol-2-amines

作　　者：曹高[1] 夏曙[2] 覃智[2] 

机构地区：[1]广东药学院医药化工学院,广东广州510006 [2]湖南大学化学化工学院,湖南长沙410082

出　　处：《今日药学》2011年第9期565-568,共4页Pharmacy Today

摘　　要：目的研究4-叔丁基-5-(1,2,4-三唑-1-基)-2-苄亚氨基噻唑类衍生物对宫颈癌细胞系Hela、肝癌细胞系Bel 7402、鼻咽癌细胞系CNE 2的体外抗癌活性。方法细胞抑制率采用四甲基偶氮唑蓝(MTT)法测定。每种试样设置5个浓度梯度(0.025、0.05、0.10、.25、0.5μmol/ml),每个浓度取4个平行样,并设置无药对照实验,用半数抑制浓度(IC50)评价目标化合物的抗癌活性。结果被测化合物对3种癌细胞均表现出一定的抑制作用,其中化合物5对Hela癌细胞和Bel 7402癌细胞的IC50值分别为0.076 1、0.062 8μmol/ml;化合物6对CNE 2癌细胞的IC50值为0.050 8μmol/ml。结论生物活性测试表明该类型氨基噻唑衍生物具有较好的抗癌活性,值得进一步研究和关注。Objective To investigation the in vitro anticancer activity of（E）-N-benzylidene-4-tert-butyl-5-（1,2,4-triazol-1-yl）thiazol-2-amines with cervical cancer cell line Hela,hepatoma cell line Bel 7402 and nasopharyngeal carcinoma cell line CNE 2.Methods The anticancer activity of the title compounds was determined by MTT colorimetry.Each sample was set 5 concentration gradients（0.025,0.05,0.1,0.25,0.5 μmol/ml）,and 4 parallel samples for each concentration.The conclusions were obtained by contrast with the control group.Results All the test compounds showed certain antitumor activities.The IC50 values of compound 5 to Hela cells and Bel 7402 cells were 0.076 1,0.062 8 μmol/ml,respectively.The IC50 values of compound 6 to CNE 2 cells was 0.050 8 μmol/ml.Conclusion The study of their biological activity shows that these 2-aminothiazole derivatives had exhibited better anticancer activity and are worth further developed.

关 键 词：4-叔丁基-5-(1 24 -三唑-1-基)-2-苄亚氨基噻唑 MTT比色法 半数抑制浓度 抗癌活性 

分 类 号：R914.5[医药卫生—药物化学]