A series of 1,3,4-oxadiazolyl benzimidazole conjugates were designed, synthesized and evaluated for their potential cytotoxicity on PC-3 prostate and MDA-MB-231 breast cancer cell lines. Some of the tested compounds displayed significant growth inhibitory activity on both cell lines, with compounds 12b and 14b showed relatively potent antitumor activity against PC-3 cells at micromolar level (IC50 = 0.36, 0.41 μM, respectively). Moreover, the potential mechanisms of the cytotoxic activity of the compound 12b on the more sensitive cell line PC-3 were studied. The result depicted that 14b was able to cause cell cycle arrest at least partly through enhancing the expression level of the cell cycle inhibitor p21 and induced cancer cell apoptosis in PC3 cell lines.

Synthesis, cytotoxic activities and cell cycle arrest profiles of benzimidazole - 1,3,4-oxadiazole conjugates

251st National Meeting (2016)

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