Synthesis, antitumor activity and SAR study of novel [1,2,4]triazino[4,5-a]benzimidazole derivatives

A series of novel 1,2,3,4-tetrahydro[1,2,4]triazino[4,5-a]benzimidazoles carrying variety of aryl and heteroaryl groups at position 1 were synthesized. The newly synthesized compounds were tested in vitro on human breast adenocarcinoma cell line (MCF7). Some of the test compounds showed potent antitumor activity, especially compound 3c [1-(2-chlorophenyl) derivative] which displayed the highest activity among the test compounds.

Graphical abstractA series of novel 1,2,3,4-tetrahydro[1,2,4]triazino[4,5-a]benzimidazoles carrying variety of aryl or heteroaryl groups at position 1 were synthesized and tested in vitro on human breast adenocarcinoma cell line (MCF7).Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► New 1-aryl-1,2,3,4-tetrahydro[1,2,4]triazino[4,5-a]benzimidazoles were synthesized. ► The newly synthesized compounds were tested in vitro on MCF7 cell line. ► Some of the test compounds showed potent antitumor activity. ► Compound 3c [1-(2-chlorophenyl) derivative] showed the highest antitumor activity.