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Synthesis and antitumor activities of 2‐(substituted)phenyl‐1,2,4‐triazolo[1,5‐a]pyridines
Authors:Guolin Zhang  Yongzhou Hu
Institution:Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, P. R. China
Abstract: chemical structure image Twenty‐three 2‐(substituted)phenyl‐1,2,4‐triazolo1,5‐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 1H 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 28μM) and compound 1w (IC50 31μM) exhibited stronger antitumor activities than cisplatin (IC50 35μM) in vitro. Hence, 1e and 1w have potential antitumor activities and are worth further investigation.
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