论文部分内容阅读
以取代苯肼盐酸盐为原料,通过Vilsmeier-Haack,Biginelli和Knoevenagel等多步反应合成了9个含有吡唑取代基的噻唑并[3,2-a]嘧啶衍生物,并利用IR,1H NMR,13C NMR,ESI-MS和HRMS对目标化合物进行了结构表征.用四甲基偶氮唑盐(MTT)法测试了目标产物对人前列腺癌PC-3细胞和人肝癌Hep G2细胞的体外抗增殖活性,部分化合物表现出了较好的生物活性,其中化合物5b,5c,5g和5i对PC-3细胞的抗肿瘤活性优于阳性对照药5-氟尿嘧啶,IC50值分别为29.98,27.69,26.36和12.56μmol/L.进一步的研究表明,化合物5i能够诱导PC-3细胞凋亡,并使其周期阻滞在G2/M期.
Nine thiazolo [3,2-a] pyrimidine derivatives containing pyrazole substituents were synthesized from substituted phenylhydrazine hydrochloride using multistep reaction of Vilsmeier-Haack, Biginelli and Knoevenagel. IR, 1H NMR, 13C NMR, ESI-MS and HRMS were used to characterize the target compounds.The target compounds were tested in vitro on human prostate cancer PC-3 cells and human hepatoma Hep G2 cells by using MTT assay Anti-proliferative activity of some compounds showed good biological activity, of which compound 5b, 5c, 5g and 5i on PC-3 cells antitumor activity superior to the positive control drug 5-fluorouracil, IC50 values were 29.98,27.69, 26.36 and 12.56μmol / L. Further studies show that compound 5i can induce PC-3 cell apoptosis, and make its cycle arrest in G2 / M phase.