含1,2-苯并噻嗪结构的咪唑并[1,2-b] [1,3,4]三氮唑衍生物的合成及其抗肿瘤活性  

Synthesis and antitumor activity of 1,2-benzothiazines imidazolo [1,2-b] [1,3,4] triazazole derivatives

作　　者：王新 赵小美 张平平 汲霞 胡国强[2] WANG Xin;ZHAO Xiaomei;ZHANG Pingping;JI Xia;HU Guoqiang(College of Pharmacy,Qilu Medical Uniersity,Zibo 255213;Institute of Pharmacy,Henan University,Kaifeng 475001,China)

机构地区：[1]齐鲁医药学院药学院,淄博255213 [2]河南大学药物研究所,开封475001

出　　处：《中国药科大学学报》2019年第5期540-543,共4页Journal of China Pharmaceutical University

基　　金：山东省高校科研计划资助项目(No.J18KB122)~~

摘　　要：以吡罗昔康甲基物为原料,利用生物电子等排等药物设计原理,合成8个结构新颖的三氮唑化合物,其结构经1H NMR、MS表征。通过测定对胰腺癌细胞Capan-1和白血病细胞L1210的抑制活性,评价目标化合物的体外抗肿瘤活性。结果表明,化合物6b(IC50=3. 6±0. 5μmol/L)对胰腺癌细胞Capan-1表现出较好的抑制活性;化合物6a(IC50=1. 8±0. 2μmol/L)对白血病细胞L1210表现出较好的抑制活性。初步的抗肿瘤活性实验结果表明,咪唑并三氮唑侧链的引入,对提高该类化合物的抗肿瘤活性有一定的作用。In this study,triazazole moiety was introduced to piroxicam,a nonsteroidal anti-inflammatory drug,via bioisosterism to produce eight target analogs,which were structurally characterized by 1H NMR and MS. These target compounds were tested for inhibitory activities on pancreatic cancer cell( Capan-1) and leukemia cell( L1210). The results showed that compound 6 b had good antiproliferative activity against Capan-1 cells( IC50=3. 6 ± 0. 5 μmol/L);while compound 6 a had good antiproliferative activity against L1210 cells( IC50= 1. 8 ± 0. 2μmol/L),indicating that the introduction of the imidazolo[1,2-b][1,3,4]triazazole moiety could be helpful to improve the antitumor activity of these compounds.

关 键 词：咪唑并[1 2-b][1 3 4]三氮唑 合成 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学] R965[医药卫生—药学]