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Issue 10, 2015
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Identification of a novel NAMPT inhibitor by combinatorial click chemistry and chemical refinement

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Abstract

The identification of compounds able to inhibit the NAD salvage pathway is experiencing a growing popularity as it has been proposed to be a novel target for antitumoral and anti-inflammatory drugs. In this manuscript, we used the copper-catalyzed [3+2] cycloaddition between azides and alkynes (click chemistry) to identify novel NAMPT inhibitors with a triazole-containing tail group. 720 compounds were synthesized in the first round, allowing the identification of 17 hit compounds. The second round of optimization brought about the discovery of compound 43 which displayed a cytotoxicity of 20 nM on neuroblastoma cancer cells and an inhibition of NAMPT of 114 nM.

Graphical abstract: Identification of a novel NAMPT inhibitor by combinatorial click chemistry and chemical refinement

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Publication details

The article was received on 19 Jun 2015, accepted on 03 Sep 2015 and first published on 07 Sep 2015


Article type: Concise Article
DOI: 10.1039/C5MD00261C
Citation: Med. Chem. Commun., 2015,6, 1891-1897
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    Identification of a novel NAMPT inhibitor by combinatorial click chemistry and chemical refinement

    S. Theeramunkong, U. Galli, A. A. Grolla, A. Caldarelli, C. Travelli, A. Massarotti, M. P. Troiani, M. A. Alisi, G. Orsomando, A. A. Genazzani and G. C. Tron, Med. Chem. Commun., 2015, 6, 1891
    DOI: 10.1039/C5MD00261C

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