Benzimidazole clubbed with triazolo-thiadiazoles and triazolo-thiadiazines: New anticancer agents

Two series of Benzimidazole clubbed with triazolo-thiadiazoles (5a–q, 5r, 5s and 5x–a1) and triazolo-thiadiazines (5t–w) were synthesized with an aim to produce promising anticancer agents. In vitro anticancer activities of synthesized compounds were investigated at the National Cancer Institute (NCI) against NCI 60 cell line panel; results showed good to remarkable broad-spectrum anticancer activity. Among them, the compound 5h (NCS: 760452, 1-(1H-benzo [d] imidazol-2-yl)-3-(6-(2,4-dichlorophenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl) propan-1-one) exhibited significant growth inhibition with GI50 values ranging from 0.20 to 2.58 μM and found superior selectivity for the leukemia cell lines and further screened at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The 5h may possibly be used as lead compound for developing new anticancer agents.

Two series of benzimidazole derivatives (5a–q, 5r, 5s, 5t–w and 5x–a1) were synthesized from 3-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-1-(1H-benzo[d]imidazol-2-yl) propan-1-one (5) and screened for their in vitro anticancer activities at the National Cancer Institute (NCI) against full NCI 60 human cell lines panel with significant results.Figure optionsDownload as PowerPoint slideHighlights
► Out of 32 new compounds 25 were selected for anti-proliferative activity by NCI.
► Initial screening of compounds showed significant to good anticancer activity.
►  Compound, 5h (NCS: 760452), exhibited remarkable anti-proliferative activity and was further screened at five dose level.
►  The 5h may be used as a template for designing and developing new anticancer agents.