Based on our previous work, a series of novel 6-arylamino-[1,2,4]triazolo[4,3-a]pyridine derivatives were synthesized, and evaluated for antiproliferative activities. SAR studies revealed that inserting an amino linkage between 6‑aryl group and [1,2,4]triazolo[4,3-a]pyridine core led to a much broader antitumor spectrum, and the most promising compound 8 l exerted potent and broad-spectrum antiproliferative activity toward HeLa, HCT116, MCF-7, and A549 cell lines, with IC₅₀ values in the micromolar range of 5.98–12.58 μM, which were more active than the positive control 5-FU. The mechanism investigation illustrated that 8 l dose-dependently caused cell cycle arrest at the G₂/M phase, and induced cell apoptosis in HeLa cells. Consequently, these findings suggest the 6-arylamino-[1,2,4]triazolo[4,3-a]pyridines afford significant potential for the discovery of a new highly efficient anticancer agents.

基于我们之前的工作，合成了一系列新型 6-芳氨基-[1,2,4]三唑并[4,3- a ]吡啶衍生物，并对其抗增殖活性进行了评估。SAR研究表明，在6-芳基和[1,2,4]三唑并[4,3- a ]吡啶核心之间插入一个氨基键会导致 更广泛的 抗肿瘤 谱，最有希望的化合物8l发挥有效和 广泛的作用。 -对 HeLa、HCT116、MCF-7 和 A549 细胞系的谱抗增殖活性，IC ₅₀值在 5.98–12.58 μM 的微摩尔范围内，比阳性对照 5-FU 更活跃。机理研究表明，8 l剂量依赖性地导致细胞周期停滞在 G ₂ /M 期，并在 HeLa 细胞中诱导细胞凋亡。因此，这些发现表明，6-芳氨基-[1,2,4]三唑并[4,3- a ]吡啶为发现新型高效抗癌剂提供了巨大的潜力。