开环Ebselen衍生物的合成、晶体结构及抑癌活性  

Synthesis,crystal structure and anticancer activities of ring-opening Ebselen derivatives

作　　者：齐凯言 冯书晓[1] 郭亚菲 王俊岭[1] 谷广娜 孙静静 付龙龙 廖源 马军营[1] QI Kai-yan;FENG Shu-xiao;GUO Ya-fei;WANG Jun-ling;GU Guang-na;SUN Jing-jing;FU Long-long;LIAO Yuan;MA Jun-ying(College of Chemical Engineering&Pharmaceutical,Henan University of Science and Technology,Luoyang 471023,China)

机构地区：[1]河南科技大学化工与制药学院,河南洛阳471023

出　　处：《化学研究与应用》2021年第7期1231-1239,共9页Chemical Research and Application

基　　金：河南省自然科学基金(182300410353)项目资助。

摘　　要：以2-氯硒基苯甲酰氯(1)为原料,通过缩合反应,合成得到开环Ebselen衍生物1a~d,其结构经^(1)H NMR,^(13)C NMR和HR-MS(ESI)表征,采用XRD测定其单晶结构。单晶X射线衍射结果表明,化合物1a~1c属于单斜晶系,P2_(1)/n空间群;化合物1d属于正交晶系,P2_(1)2_(1)2_(1)空间群。并通过MTT法考察了这些化合物对食管癌细胞(EC109)的体外增殖抑制活性。结果表明,在浓度为100μg·mL^(-1)时,化合物1c具有较强的抑制EC109细胞增殖的活性,抑制率为29.55%。With 2-chloroselenium-benzoyl chloride(1)as raw material,synthesis of ring-opening Ebselen derivatives 1a~d.The structures were characterized by ^(1)H NMR,^(13)C NMR and HR-MS(ESI),and the molecular structure was determined by XRD.The result of single crystal X-ray diffraction shows that compounds 1a~c belongs to the monoclinic system and P2_(1)/n space group,compound 1d belongs to the orthorhombic system and P2_(1)2_(1)2_(1) space group.The inhibitory activity of these compounds to the proliferation of esophageal cancer cells(EC109)in vitro was investigated by MTT assay.The results showed that compound 1c had a strong inhibitory effect on EC109 cell proliferation at the concentration of 100μg·mL^(-1),and the inhibitory rate was 29.55%.

关 键 词：2-氯硒基苯甲酰氯 晶体结构 抑癌活性 食管癌细胞(EC109) 

分 类 号：O641.4[理学—物理化学]