噻吩并吡啶酰胺类化合物的设计、合成及抗肿瘤活性研究  

Design,Synthesis and Antitumor Activity of Thiophenopyridine Amide Compounds

作　　者：汤泉 TANG Quan(Public Basic College,Bengbu Medical College,Bengbu 233030,China)

机构地区：[1]蚌埠医学院公共基础学院,安徽蚌埠233030

出　　处：《长春师范大学学报》2021年第6期57-61,共5页Journal of Changchun Normal University

基　　金：安徽省高校自然科学研究项目“新型四氢异喹啉靶向抗肿瘤药物的设计、合成及活性筛选”(KJ2019A0390)。

摘　　要：依据药物拼合原理,本文设计了3个噻吩并吡啶酰胺类化合物,以取代苯甲醛、4,5,6,7-四氢噻吩并[3,2-c]吡啶、N,N-二甲基氯丙烷等为原料,通过Knoevenagel反应、酰胺化反应、亲核取代反应等步骤对设计化合物进行了合成,3个噻吩并吡啶酰胺类化合物的结构均经^(1)H-NMR佐证。采用SRB法测试了所合成的3个化合物的抗肿瘤活性,化合物6a、6b、6c对A549肿瘤细胞的抑制活性与5-氟尿嘧啶相当。According to combination principles,three thiophenopyridine amide compounds were designed.They were synthesized by Knoevenagel reaction,acylation reaction and nucleophilic substitution reaction.And the materials were substituted benzaldehyde,4,5,6,7-tetrahydrothiopheno[3,2-c]pyridine and N,N-dimethylchloropropane.The structures of three thiophenopyridine amide compounds were identified by ^(1)H-NMR.The targets compounds were tested for antitumor activity by SRB method.The inhibitory activity of compounds 6a,6b and 6c on A549 cells was similar to that of 5-fluorouracil.

关 键 词：噻吩并吡啶 苯丙烯酸 抗肿瘤 

分 类 号：O622[理学—有机化学]