A series of [1,2,3]triazolo[4,5-d]pyrimidine derivatives bearing a hydrazone moiety were designed, synthesized and evaluated for their antiproliferative activity against several cancer cell lines of different origins by MTT assay. Most of the synthesized compounds demonstrated moderate to good activity against the cancer cell lines selected. Especially, compound 43 showed the most potent antiproliferative activity as well as good selectivity between cancer and normal cells (IC₅₀ values of 0.85 μM against MGC-803 and 56.17 μM against GES-1). In addition, compound 43 evidently inhibited the colony formation of MGC-803 cells at 0.8 μM. Further mechanism studies revealed that compound 43 could induce apoptosis of MGC-803 cells probably through the mitochondrial pathway accompanied with decrease of the mitochondrial membrane potential (MMP), activations of caspase-9/3, up-regulation of the expression of Bax, Bak and PUMA, as well as down-regulation of that of Bcl-2 and Mcl-1.

设计，合成了一系列带有部分的[1,2,3]三唑并[4,5- d ]嘧啶衍生物，并通过MTT分析评估了其对几种不同来源的癌细胞系的抗增殖活性。大多数合成的化合物显示出对所选癌细胞系中等至良好的活性。尤其是，化合物43在癌细胞与正常细胞之间显示出最有效的抗增殖活性以及良好的选择性（针对MGC-803的IC ₅₀值为0.85μM，针对GES-1的IC ₅₀值为56.17μM）。另外，化合物43明显地抑制了0.8μM的MGC-803细胞的集落形成。进一步的机理研究表明，化合物43 可能通过线粒体途径诱导MGC-803细胞凋亡，伴随线粒体膜电位（MMP）降低，caspase-9 / 3活化，Bax，Bak和PUMA表达上调以及下调-对Bcl-2和Mcl-1的调节。