Five series of N-methylpicolinamide moiety and thienopyrimidine moiety bearing triazole (21–26, 27–34, 35–41, 42–47 and 48–54) were designed and synthesized. And all the target compounds were evaluated for the IC₅₀ values against three cancer cell lines (A549, HepG2 and MCF-7) and some selected compounds (43, 49 and 52) were further evaluated for the activity against c-Met, Flt-3, VEGFR-2, c-Kit and EGFR kinases. Moreover, SARs and docking studies indicated that thieno[3,2-d]pyrimidine bearing triazole moiety was privileged structure for the activity. Especially, the Cl atom on the 4-C position of aryl group showed the best activity. The most promising compound 49 showed 3.7–5.4-fold more activity than the lead drug Foretinib against A549, HepG2 and MCF-7 cell lines, with the IC₅₀ values of 0.9 ± 0.1 µM, 0.5 ± 0.1 µM and 1.1 ± 0.2 µM, respectively. And The experiments of enzyme-based showed that 49 inhibitor the c-Met selectively, with the IC₅₀ values of 16 nM, which showed equal activity to Foretinib (14 nM). What’s more, According to the result of AO single staining and Annexin V/PI staining, it's claimed that the 49 could induce late apoptosis of HepG2 cells and by a concentration-dependent manner.

五个系列的N-甲基吡啶酰胺部分和噻吩并嘧啶基部分轴承三唑（21-26，27-34，35-41，42-47和48-54）设计并合成。和所有的目标化合物为IC评价₅₀对三名癌细胞系（A549，HepG2和MCF-7）和一些选择的化合物（值43，49和52），用于针对c-Met的，FLT-活性中进一步评估3，VEGFR-2，c-Kit和EGFR激酶。而且，合成孔径雷达和对接研究表明，thieno [3,2- d带有]嘧啶的三唑部分是该活性的优先结构。特别地，芳基的4-C位置上的Cl原子显示出最佳活性。最有前途的化合物49对A549，HepG2和MCF-7细胞系的活性比前药Foretinib高3.7-5.4倍，IC ₅₀值为0.9±0.1 µM，0.5±0.1 µM和1.1±0.2 µM，分别。并且基于酶的实验表明，49种选择性抑制c-Met的药物，IC ₅₀值为16 nM，与Foretinib（14 nM）具有相同的活性。此外，根据AO单一染色和Annexin V / PI染色的结果，据称49 可以通过浓度依赖性的方式诱导HepG2细胞的晚期凋亡。