Abstract

Twenty new 3,6-disubstituted-1,2,4-triazine derivatives containing benzimidazole moiety (4) were synthesized via microwave-assisted condensation reactions of 2-aryloxymethylbenzimidazole-1-acetylhydrazines (3) with various (un)substituted phenacyl bromides in DMF. The structures were characterized by IR, 1 H NMR spectra and elemental analysis. The optimum experimental conditions were found. Compared with traditional methods, this synthetic method has such advan- tages as short reaction time, simple operation, broad substrate scope, easy purification and high yields. The synthesized target compounds were screened for Cdc25B and PTP1B inhibitory activities. The experimental results indicate that compounds 4g and 4j showed good inhibitory activities against Cdc25B, and 4a, 4h, 4j, 4r and 4s exhibited potent inhibitory activities against PTP1B. It is noteworthy that compound 4j can be used as potential Cdc25B and PTP1B inhibitors in the treatment of cancer and diabetes. Keywords microwave irradiation; 1,2,4-triazines; benzimidazole; synthesis; Cdc25B and PTP1B inhibitors

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