摘要
目的:设计合成一系列正丁酸水杨酰芳胺酯类化合物并考察其体外抗肿瘤活性。方法:以不同的水杨酸与芳胺为原料经3步反应得到目标化合物;以K562,A549,A431细胞为靶细胞,MTT法与SRB法进行初步的体外抗肿瘤活性研究。结果与结论:合成了12个目标化合物,其结构经IR,1H-NMR,13C-NMR及MS确证。目标化合物对3种细胞株均具有不同程度的抑制活性,其中化合物6c,6f,6l抑制活性强于阳性对照药吉非替尼,与原药氯硝柳胺相当。
Objective： To design and synthesize a series of n-butyric acid salicylanilide esters,and to determine their anti-tumor activity.Methods： Different salicylic acids and aromatic amines were used as starting materials to synthesize target compounds through 3 steps.Anti-tumor activities of these compounds in K562,A549,A431 cells in vitro were investigated by MTT assay and SRB assay.Results and Conclusion： Twelve compounds were synthesized.Their structures were confirmed by IR,1H-NMR,13C-NMR and MS.The target compounds exhibited antitumor activities in these cells lines,and compounds 6c,6f,6l were found to have stronger cell growth inhibitory than gefitinib,and comparable to niclosamide.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2013年第14期1684-1690,1696,共8页
Chinese Journal of New Drugs
基金
安徽省自然科学基金(1208085MH128)
关键词
正丁酸
水杨酰芳胺
抗肿瘤活性
合成
n-abutyric acid
salicylanilide
antitumor activity
synthesis
