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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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Supplementary files

Article information


Submitted
19 Jun 2015
Accepted
03 Sep 2015
First published
07 Sep 2015

Med. Chem. Commun., 2015,6, 1891-1897
Article type
Concise Article

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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