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

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.