Ishan I Panchal, Animesh G. Devgirkar, Ashish D. Patel
Jan 21, 2020
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Abstract
The treatment of cancer requires scientific advancement. ATP-competitive mTOR inhibitors have been studied as potential antitumor agents. 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. 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. 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. 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.