1443232-08-3

Upstream product

• 122502-94-7 2-(1H-benzo[d][1,2,3]triazol-1-yl)acetohydrazide 
• 69218-46-8 ethyl (1H-benzotriazol-1-yl)acetate 
• 95-14-7 1,2,3-Benzotriazole 
• 136715-68-9 5-((1H-benzo[d][1,2,3]triazol-1-yl)methyl)-1,3,4-oxadiazole-2-thiol 
• 589-15-1 1-bromomethyl-4-bromobenzene 

Relevant academic research and scientific papers

Synthesis, biological evaluation, and molecular docking studies of novel 1,3,4-oxadiazole derivatives possessing benzotriazole moiety as FAK inhibitors with anticancer activity

1,3,4-Oxadiazole derivatives have drawn continuing interest over the years because of their varied biological activities. In order to search for novel anticancer agents, we designed and synthesized a series of new 1,3,4-oxadiazole derivatives containing benzotriazole moiety as potential focal adhesion kinase (FAK) inhibitors. All the synthesized compounds were firstly reported. Among the compounds, compound 4 shows the most potent inhibitory activity against MCF-7 and HT29 cell lines with IC50 values of 5.68 μg/ml and 10.21 μg/ml, respectively. Besides, all the compounds were assayed for FAK inhibitory activity using the TRAP-PCR-ELISA assay. The results showed compound 4 exhibited the most potent FAK inhibitory activity with IC50 values of 1.2 ± 0.3 μM. Docking simulation by positioning compound 4 into the FAK structure active site was performed to explore the possible binding mode. Apoptosis which was analyzed by flow cytometry, demonstrated that compound 4 induced apoptosis against MCF-7 cells. Therefore, compound 4 may be a potential anticancer agent against MCF-7 cancer cell.