【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~1H-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。更多还原

【Abstract】 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 ~1H-NMR. The targets compounds were tested for antitumor activity by SRB method. The inhibitory activity of compounds 6 a, 6 b and 6 c on A549 cells was similar to that of 5-fluorouracil.更多还原