Journal
MEDCHEMCOMM
Volume 6, Issue 10, Pages 1891-1897Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5md00261c
Keywords
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Funding
- AIRC [IG10509, 14832]
- Fondazione San Paolo
- Italian Ministry of Education [PRIN-2010W7YRLZ_002]
- Department of Pharmaceutical Sciences
- Angelini Research Center
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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.
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