Background: The treatment of cancer requires scientific advancement. ATP-competitive mTOR
inhibitors have been studied as potential antitumor agents.
Objective: A series of substituted benzimidazole compounds were designed, synthesized and characterized via
introducing 2-chloroquinolin into 2nd position and most title compounds exhibited enhanced anticancer activities.
Methods: To study the anticancer mechanism, VIa-VIh was successfully docked by iGEMDOCK 2.0
which gives good affinity towards m-TOR/PI3K dual inhibitors. The anti-proliferative activities of these
compounds were evaluated on MCF-7 and A549 cell line for Breast and lung cancer, respectively.
Results: 2-(2-chloroquinolin-3-yl)-1H-benzoimidazol-1-yl)(phenyl)methanone (VIa) exhibited significant
anti-proliferative activity, especially against breast cancer (IC50 197 μM) for MCF7 cell line and (2-(2-
chloroquinolin-3-yl)-1H-benzo[d]imidazol-1-yl)(4-nitrophenyl)methanone (VIc) was significantly active
against lung cancer (IC50 89 μM) for A579 cell line.
Conclusion: VIa gives more activity on breast cancer and it gives IC50 197 μM for MCF7 cell line and (2-
(2-chloroquinolin-3-yl)-1H-benzo[d]imidazol-1-yl) (4-nitrophenyl) methanone (VIc) lung cancer IC50 89
μM for A579 cell line.