Synthesis, characterization and cytotoxic activity evaluation of 4-(1,2,3-triazol-1-yl) salicylic acid derivatives

Abstract A novel series of 4-(1,2,3-triazol-1-yl) salicylic acid derivatives was synthesized from 4-azidosalicylic acid and diverse alkynes using copper catalyzed azide-alkyne cycloaddition as key process and fully characterized by using different analytical techniques. The in vitro antiproliferative activity of these new compounds was explored against a series of tumoral cell lines which included U251 (human glioblastoma), PC-3 (human prostate cancer cell line), K562 (human leukemia), HCT-15 (human colorectal adenocarcinoma), MCF-7 (human breast adenocarcinoma) and SKLU (human lung adenocarcinoma), showing selective activity in some compounds. Moreover, molecular docking studies suggest a strong interaction between ARG-154 in STAT3 and the triazole fragment which can explain the inhibitory activity observed in these compounds.