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Issue 11, 2016
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Potent sirtuin inhibition with 1,2,5-trisubstituted benzimidazoles

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Abstract

Two series of compounds were synthesized based on the benzimidazole scaffold. The compounds were subsequently screened for their SIRT1, SIRT2 and SIRT3 activities. Three of the compounds showed good inhibitory activity against SIRT2 in this study with the most potent compound (5i) having an IC50 value of 2.9 μM. Molecular docking analysis demonstrated that 5i was able to inhibit SIRT2 by displacing the co-factor NAD+ in the active site. This was further confirmed experimentally by ligand-NAD+ competitive assay.

Graphical abstract: Potent sirtuin inhibition with 1,2,5-trisubstituted benzimidazoles

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Publication details

The article was received on 08 Jul 2016, accepted on 03 Aug 2016 and first published on 05 Aug 2016


Article type: Research Article
DOI: 10.1039/C6MD00378H
Citation: Med. Chem. Commun., 2016,7, 2094-2099
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    Potent sirtuin inhibition with 1,2,5-trisubstituted benzimidazoles

    Y. K. Yoon, H. Osman and T. S. Choon, Med. Chem. Commun., 2016, 7, 2094
    DOI: 10.1039/C6MD00378H

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