Novel Fluorinated Benzimidazole-Based Scaffolds and their Anticancer Activity in vitro
A small library of twelve, structurally diverse, fluoroaryl benzimidazoles was prepared using a simple synthetic strategy employing SNAr reactions. This allowed rapid assembly of heterocyclic structures containing linked and tethered fluoroaryl benzimidazoles. X-ray crystal structures of seven compounds were obtained including those of two macrocyclic compounds containing 21- and 24-membered rings. Three tethered fluoroaryl benzimidazole derivatives demonstrated micromolar inhibition against K-562 and MCF-7 cell lines. These compounds, in addition to 1-tetrafluoropyrid-4-yl-2-tetrafluoropyrid-4-ylsulfanyl-1H-benzimidazole, also demonstrated micromolar inhibition against G361 and HOS cell lines. Two of the compounds were found to activate caspases leading to apoptosis.
The file attached to this record is the author's final peer reviewed version. The Publisher's final version can be found by following the DOI link.
Citation : Bhambra, A.S. et al. (2016) Novel Fluorinated Benzimidazole-Based Scaffolds and their Anticancer Activity in vitro. Journal of Fluorine Chemistry, 188, pp. 99-109
Research Group : Biomedical and Environmental Health
Research Institute : Institute for Allied Health Sciences Research
Peer Reviewed : Yes