含噻吩片段的三嗪类化合物的合成与抗肿瘤活性研究  

Synthesis and Antitumor Activity of Triazines Containing Thiophene Fragments

作　　者：饶念 龙志武 乐意[1] 刘力[1] 鄢龙家 RAO Nian;LONG Zhi-wu;LE Yi;LIU Li;YAN Long-jia(School of Pharmaceutical Sciences,Guizhou University,Guiyang 550025,China)

机构地区：[1]贵州大学药学院,贵州贵阳550025

出　　处：《化学试剂》2023年第4期81-90,共10页Chemical Reagents

基　　金：贵州省科技计划项目(黔科合基础-ZK[2022]一般124)。

摘　　要：以3-氨基噻吩-2-羧酸甲酯为原料设计合成了一系列含噻吩片段的结构新颖的三嗪类化合物。最终的22个化合物结构经1HNMR,13 CNMR和HRMS确证。并且用MTT法评价了该系列化合物对人脑恶性星形胶质母细胞瘤细胞U87-MG的体外抗肿瘤活性。结果表明,化合物3-((4-氯-6-((4-(甲基磺酰基)苯基)氨基)-1,3,5-三嗪-2-基)氨基)-N-甲基噻吩-2-甲酰胺具有良好的抗肿瘤活性且优于阳性对照TAE-226,其对人脑恶性星形胶质母细胞瘤细胞U87-MG的IC 50为9.528μmol。此研究以期为含1,3,5-三嗪骨架的抗肿瘤药物提供参考。A series of novel triazines containing thiophene fragments were designed and synthesized from 3-aminothiophene-2-carboxylic acid methyl ester.The structures of the final 22 compounds were confirmed by 1HNMR,13 CNMR and HRMS.The anti-tumor activity of these compounds against human brain malignant astroblastoma cell line U87-MG in vitro was evaluated by MTT assays.The results showed that the compound 3-((4-chloro-6-((4-(methylsulfonyl)phenyl)amino)-1,3,5-triazin-2-yl)amino)-N-methylthiophene-2-carboxamide had very good anti-tumor activity and was superior to the positive control TAE-226.Its IC 50 to human malignant astroblastoma cell U87-MG is 9.528μmol.This study was expected to provide guidance for anti-tumor drugs containing 1,3,5-triazine skeleton.

关 键 词：噻吩 三嗪 抗肿瘤 合成 MTT法 

分 类 号：R914[医药卫生—药物化学]