Synthesis and antitumor activities of 2-(substituted)phenyl-1,2,4-triazolo[1,5-a]pyridines

摘要

Twenty-three 2-(substituted)phenyl-1,2,4-triazolo[1,5-a]pyridines have been synthesized by cycloadditison reaction between N-amino methylpyridinium mesitylenesulfonates and substituted benzonitriles under the presence of potassium hydroxide at room temperature. The structures of all products were confirmed by H-1 NMR, MS and elemental analyses. The antitumor activities of these compounds were evaluated against human ovary cancer cell line (HO-8910) in vitro by MTT method. The preliminary results showed that compound 1e (IC50 28 mu M) and compound 1w (IC50 31 mu M) exhibited stronger antitumor activities than cisplatin (IC50 35 mu M) in vitro. Hence, le and 1w have potential antitumor activities and are worth further investigation.