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

✍ Scribed by Guolin Zhang; Yongzhou Hu


Publisher
Journal of Heterocyclic Chemistry
Year
2007
Tongue
English
Weight
232 KB
Volume
44
Category
Article
ISSN
0022-152X

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✦ Synopsis


Abstract

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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 ^1^H 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 (IC~50~ 28ΞΌM) and compound 1w (IC~50~ 31ΞΌM) exhibited stronger antitumor activities than cisplatin (IC~50~ 35ΞΌM) in vitro. Hence, 1e and 1w have potential antitumor activities and are worth further investigation.


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Synthese von 2H-1,2,3-Triazolo[4,5-~][1,2,4]triazolo[4,3-a]pyridinen und verwandten Systemen Zur Herstellung des 2H-1,2,3-Triazolo[4,5-c]pyridin-4(5H)-ons 4 wurde 2-Phenyl-2H-l,2,3triazol-4-carbaldehyd (1) zunichst in die Acrylsiiure 2 umgewandelt und letztere dann nach vorausgehender Curtius-Umlage