Novel Fluorinated Benzimidazole-Based Scaffolds and their Anticancer Activity in vitro

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dc.cclicenceCC-BY-NC-NDen
dc.contributor.authorBhambra, Avninder S.en
dc.contributor.authorEdgar, Marken
dc.contributor.authorElsegood, Mark R. J.en
dc.contributor.authorHorsburgh, Lynneen
dc.contributor.authorKryštof, Vladimiren
dc.contributor.authorLucas, Paul D.en
dc.contributor.authorMojally, Mariamen
dc.contributor.authorTeat, Simon J.en
dc.contributor.authorWarwick, Thomas G.en
dc.contributor.authorWeaver, George W.en
dc.contributor.authorZeinali, Fatemehen
dc.date.acceptance2016-06-17en
dc.date.accessioned2016-07-22T09:09:05Z
dc.date.available2016-07-22T09:09:05Z
dc.date.issued2016-06-23
dc.descriptionThe 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.en
dc.description.abstractA 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.en
dc.funderN/Aen
dc.identifier.citationBhambra, A.S. et al. (2016) Novel Fluorinated Benzimidazole-Based Scaffolds and their Anticancer Activity in vitro. Journal of Fluorine Chemistry, 188, pp. 99-109en
dc.identifier.doihttps://doi.org/10.1016/j.jfluchem.2016.06.009
dc.identifier.urihttp://hdl.handle.net/2086/12330
dc.language.isoenen
dc.peerreviewedYesen
dc.projectidN/Aen
dc.publisherElsevieren
dc.researchgroupBiomedical and Environmental Healthen
dc.researchinstituteInstitute for Allied Health Sciences Researchen
dc.subjectAnticanceren
dc.subjectDrug discoveryen
dc.subjectin vitroen
dc.subjectBenzimidazoleen
dc.subjectFluorineen
dc.subjectSNARen
dc.titleNovel Fluorinated Benzimidazole-Based Scaffolds and their Anticancer Activity in vitroen
dc.typeArticleen

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