6-[2-(1,2,4,5-四嗪-3-基)肼基]-1,3,5-三嗪类化合物的合成和抗肿瘤活性研究

Synthesis and antitumor activities of 6-( 2-(1,2,4,5-tetrazin-3-yl) hydrazinyl)-1,3,5-triazine derivatives

以3,6-二(3,5-二甲基-1H-吡唑-1-基)-1,2,4,5-四嗪为原料,与水合肼反应,得到3-取代-6-肼基-1,2,4,5-四嗪,进一步与三聚氯氰和胺反应,得到6-[2-(1,2,4,5-四嗪-3-基)肼基]-1,3,5-三嗪类化合物,通过元素分析、1H NMR、IR和MS对这些化合物进行了表征;并进一步将此类化合物进行体外人绒毛膜癌细胞株Bewo、子宫内膜癌细胞株Ishikawa、人肺癌细胞株A549、人乳腺癌细胞株MCF-7、人白血病细胞株HL-60的测试,以顺铂为对照,发现此类化合物具有一定的体外抗肿瘤活性,值得进一步研究。

3-Substituted-6-hydrazinyl-1,2,4,5-tetrazines were prepared from 3,6-bis （ 3,5-dimethyl-1 h- pyrazol-1-yl）- 1,2,4,5-tetrazine and hydrazine hydrate, which were further reacted with cyanuric chloride and amide to yield 6-（ 2-（ 1, 2,4,5-tetrazin-3-yl） hydrazinyl） -1,3,5-triazines. These synthesized compounds were characterized by 1H NMR, MS,IR and element analysis and evaluated for their in vitro anticancer activities against Bewo, Ishikawa, A549, MCF-7, found them with a certain anticancer activities in vitro, so tial antitumor activities and is worth to research further. HL-60 cell lines （cisplatin as a control）, and it is a kind of compound which possesses potential antitumor activities and is worth to research further.