1λ^(4)-1,1′-螺环[3H-2,1-苯并噁硒醇]-3,3′-二酮的合成、结构表征及其抗肿瘤活性  

Synthesis,structure characterization and antitumor activity of1λ^(4)-1,1′-Spirobi[3H-2,1-benzoxaselenole]-3,3′-dione

作　　者：赵鹏宇 冯书晓[1] 曹泽林 王开开 刘博宽 李念祖 李宜衡 马军营[1] ZHAO Peng-yu;FENG Shu-xiao;CAO Ze-lin;WANG Kai-kai;LIU Bo-kuan;LI Nian-zu;LI Yi-heng;MA Jun-ying(College of Chemical Engineering&Pharmaceutical,Henan University of Science and Technology,Luoyang 471000,China;Agricultural College/Peony College,Henan University of Science and Technology,Luoyang 471000,China)

机构地区：[1]河南科技大学化工与制药学院,河南洛阳471000 [2]河南科技大学农学院/牡丹学院,河南洛阳471000

出　　处：《化学研究与应用》2022年第6期1316-1320,共5页Chemical Research and Application

基　　金：河南省自然科学基金资助项目(182300410353)资助;国家级大学生创新创业训练计划项目(202010464067)资助;河南科技大学大学生研究训练计划(SRTP)项目(2021364)资助。

摘　　要：选用原料为2-氯硒基苯甲酰氯,合成了1λ^(4)-1,1′-螺环[3H-2,1-苯并噁硒醇]-3,3′-二酮(2),其结构经1H NMR、^(13)C NMR和HR-MS(ESI)表征,采用XRD测定其单晶结构。结果为:2(CCDC:2103256)属单斜晶系,C2/c空间群,晶胞参数为a=13.6501(5)A,b=8.6273(3)A,c=10.0389(5)A,β=96.718(4)°,V=1174.11(8)A^(3),Z=4,D c=1.806 g·cm^(-3),F(000)=632.0,R_(gt)(F)=0.0280,wR ref(F^(2))=0.1172,S=1.083,μ=4.422 mm^(-1)。用MTT法评价了标题化合物2对五种常见癌细胞毒株体外增殖的抑制活性。结果表明,常见抑癌物质相比,2抑制活性提高明显。With 2-chloroselenium-benzoyl chloride as raw material,1λ^(4)-1,1′-Spirobi[3H-2,1-benzoxaselenole]-3,3′-dione(2)was synthesized.The structure were characterized by ^(1)H NMR,^(13)C NMR and HR-MS(ESI),and the molecular structure was determined by XRD.The results showed that 2(CCDC:2103256)belong to monoclinic system,space group C2/c,and the unit cell parameters were a=13.6501(5)A,b=8.6273(3)A,c=10.0389(5)A,β=96.718(4)°,V=1174.11(8)A^(3),Z=4,Dc=1.806 g·cm^(-3),F(000)=632.0,R_(gt)(F)=0.0280,wR_(ref)(F^(2))=0.1172,S=1.083,μ=4.422 mm^(-1).MTT assay was used to evaluate the inhibitory activity of compound 2 on the proliferation of five common cancer cells in vitro.The results showed that the antitumor activity of 2 was significantly higher than that of common antitumor substances.

关 键 词：有机硒化合物 合成 晶体结构 抗肿瘤活性 MTT法 

分 类 号：O626[理学—有机化学]