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Synthesis and antitumor activities of 2-(substituted)phenyl-1,2,4-triazolo[1,5-a]pyridines
β 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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β¦ Synopsis
Abstract
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Twentyβthree 2β(substituted)phenylβ1,2,4βtriazolo[1,5βa]pyridines have been synthesized by cycloadditison reaction between Nβamino 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 (HOβ8910) 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.
π SIMILAR VOLUMES
## Abstract The synthesis of nine novel triazolopyridines (I) bearing pyrrolidine, piperidine, piperazine and morpholine heterocyclic appendages is reported.
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