Molecular Modelling, Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives for the Treatment of Breast Cancer

(E-pub Ahead of Print)

Author(s): Ishan Panchal*, Animesh G. Devgirkar, Ashish D Patel, Afzal Nagani, Chaitali Lad

Journal Name: Current Chinese Chemistry

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Background: The treatment of cancer must be needed with the 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 by on MCF-7 and A549 cell line for Brest and lung cancer respectively. Results: 2-(2-chloroquinolin-3-yl)-1H-benzoimidazol-1-yl)(phenyl)methanone (VIa) exhibited significant anti-proliferative activity, especially against brest 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.

Keywords: m-TOR/PI3K, A579 , benzimidazole , MCF-7, A549, iGEMDOCK 2.0

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(E-pub Ahead of Print)
DOI: 10.2174/2666001601666200121163605