2-(2-取代-1,3,4-噻二唑-5-基)-苯并异硒唑-3(2H)-酮衍生物的合成及体外抗癌活性  

Synthesis and Antitumor Activity of 2-(2-Substituted 1,3,4-thiadiazol-5-yl)benzisoselenazol-3(2H)-one Derivatives

作　　者：史艳萍[1] 陈宝泉[1] 麻静[1] 刘玉明[1] 李彩文[1] 

机构地区：[1]天津理工大学化学化工学院,天津300384

出　　处：《化学学报》2011年第21期2561-2566,共6页Acta Chimica Sinica

基　　金：国家自然科学基金(No.20971097)资助项目

摘　　要：根据活性基团拼合原理,用2-氯硒基苯甲酰氯和2-氨基-5取代-1,3,4-噻二唑缩合合成了10个新的2-(2-取代-1,3,4-噻二唑-5-基)-苯并异硒唑-3(2H)-酮衍生物(6),并通过IR,1H NMR,ESI-MS和元素分析对其结构进行了确认,采用CCK-8法测试了化合物抑制肿瘤细胞增殖活性.结果表明,化合物6h对人体肺癌细胞A-549,化合物6a,6b,6d,6e,6f,6g,6h,6j对人体乳腺癌细胞MCF-7,化合物6a,6b,6d,6e,6f,6g对人体肝癌细胞SSMC-7721抑制活性均强于阳性对照药依布硒啉,且表现出一定的选择性,具有进一步研究的潜在价值.Ten novel 2-（2-substituted 1,3,4-thiadiazol-5-yl）benzisoselenazol-3（2H）-one derivatives（6） were synthesized by the condensation of 2-chloroselenobenzoyl chloride and 2-amino-5-substituted 1,3,4-thiadiazole according to substructure link principle,and structurally confirmed by IR,1H NMR,ESI-MS techniques and elemental analysis.The antiproliferative activities against three tumor cells were tested using CCK-8 method.The results indicated that 6h against A-549,6a,6b,6d,6e,6f,6g,6h,6j against MCF-7 and 6a,6b,6d,6e,6f,6g against SSMC-7721 showed better activities than positive control Ebselen did,which suggested such compounds with a certain selectivity to the three tumor cells and were worth further investigation.

关 键 词：硒 苯并异硒唑酮 1 3 4-噻二唑 合成 抗癌活性 

分 类 号：R914[医药卫生—药物化学] O627.61[医药卫生—药学]