1,2,3-三唑类化合物的合成及其体外抗肿瘤活性

Synthesis of 1,2,3-triazoles and their antitumor activities in vitro

以多孔铜为催化剂,通过卤代烃与端位炔烃及叠氮化钠Click反应,一锅法合成了6个1,4-取代的1,2,3-三唑化合物,其结构经1H NMR,13C NMR,IR和HR-MS表征。采用MTT法初步研究该类化合物对肿瘤细胞株的增殖抑制活性,结果表明化合物3e和3f具有一定的抗肿瘤活性,但均低于顺铂。

1,2,3-Triazoles were synthesized using porous Cu as a catalyst via one-pot multi component reaction from alkynes, alkyl halides, and sodium azide. The structures were characterized by NMR, IR and HR-MS. Antitumor activities against cell line MCF-7, A549 and HL-60 were tested by MTT method. The results shown that compound 3e and 3f possessed certain antitumor activity, however, their activity was weaker than cis-dichlorodiamineplatinum（II）.