含噻唑与三唑酮结构衍生物的合成及其抗肿瘤活性

Synthesis and antitumor activity of derivatives containing thiazole and triazolone structure

[目的]合成一系列含吡唑环的噻唑与三唑酮稠杂环结构的衍生物并测定其抗肿瘤活性.[方法]以异烟酸为起始原料合成21个含噻唑与三唑酮稠杂环结构的一系列衍生物,经1 H NMR和13C-NMR验证其结构,利用MTT法检测所有化合物对8种人来源癌细胞和人正常肝细胞的抗增殖活性.[结果]大部分化合物的抗增殖活性均强于对照药DDP,其中化合物5p和5q对8种人癌细胞株的抑制增殖活性均较好,特别是化合物5q对人胃癌细胞SGC-7901的抗增殖活性最强,其IC50值为(41.5±13.6)μmol/L.[结论]化合物5q具有良好的后续研究价值.

OBJECTIVE To synthesize a series of derivatives with thiazole containing pyrazole ring and triazolone containing thick heterocyclic ring structure and evaluate their antitumor activities.METHODS21 derivatives containing thiazole and triazolone structure were synthesized from isonicotinic acid as starting material,and their structures were verified by 1 H-NMR and 13 C-NMR.MTT assay was used to detect the anti-proliferation activities of all compounds against 8 human cancer cell lines and human normal liver cells.RESULTS The anti-proliferation activity of most compounds was stronger than that of the control drug DDP.Among them,compounds 5 p and 5 q had good inhibitory effects on 8 human cancer cell lines.Especially the compound 5 q had the most potent anti-proliferation activity against the human gastric cancer cell SGC-7901,and the IC50 value was 41.5±13.6.μmol/L.CONCLUSION Compound 5 q had good value for further research.