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Novel fluorinated benzimidazole-based scaffolds and their anticancer activity in vitro

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389030%3A_____%2F16%3A00463793" target="_blank" >RIV/61389030:_____/16:00463793 - isvavai.cz</a>

  • Alternative codes found

    RIV/61989592:15310/16:33161109

  • Result on the web

    <a href="http://dx.doi.org/10.1016/j.jfluchem.2016.06.009" target="_blank" >http://dx.doi.org/10.1016/j.jfluchem.2016.06.009</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.jfluchem.2016.06.009" target="_blank" >10.1016/j.jfluchem.2016.06.009</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Novel fluorinated benzimidazole-based scaffolds and their anticancer activity in vitro

  • Original language description

    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-4ylsulfanyl-1H-benzimidazole, also demonstrated micromolar inhibition against G361 and HOS cell lines. Two of the compounds were found to activate caspases leading to apoptosis.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    FR - Pharmacology and apothecary chemistry

  • OECD FORD branch

Result continuities

  • Project

    <a href="/en/project/GA15-15264S" target="_blank" >GA15-15264S: Targeted Transport of Purine Cyclin-dependent Kinase Inhibitors into Cancer Cells</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2016

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Journal of Fluorine Chemistry

  • ISSN

    0022-1139

  • e-ISSN

  • Volume of the periodical

    188

  • Issue of the periodical within the volume

    AUG

  • Country of publishing house

    CH - SWITZERLAND

  • Number of pages

    11

  • Pages from-to

    99-109

  • UT code for WoS article

    000381836000016

  • EID of the result in the Scopus database