Open AccessMolecular Modelling, Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives for the Treatment of Breast Cancer
Author(s) -
Ishan Panchal,
G. Devgirkar Animesh,
Ashish Patel,
Afzal Nagani,
Lad Chaitali
Publication year - 2021
Publication title -
current chinese chemistry
Language(s) - English
Resource type - Journals
eISSN - 2666-0016
pISSN - 2666-0008
DOI - 10.2174/2666001601666200121163605
Subject(s) - benzimidazole , ic50 , mcf 7 , chemistry , breast cancer , lung cancer , cell culture , stereochemistry , cancer , pharmacology , cancer research , in vitro , biochemistry , human breast , medicine , oncology , biology , organic chemistry , genetics
Background: The treatment of cancer requires scientific advancement. ATP-competitive mTORinhibitors have been studied as potential antitumor agents. Objective: A series of substituted benzimidazole compounds were designed, synthesized and characterized viaintroducing 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 2.0which gives good affinity towards m-TOR/PI3K dual inhibitors. The anti-proliferative activities of thesecompounds 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 significantanti-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 activeagainst 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 89μM for A579 cell line.