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Identification of Novel Triazole-Based Nicotinamide Phosphoribosyltransferase (Nampt) Inhibitors Endowed With Antiproliferative and Antiinflammatory Activity Publisher Pubmed



Travelli C1 ; Aprile S1 ; Rahimian R2, 3 ; Grolla AA1 ; Rogati F1 ; Bertolotti M1 ; Malagnino F1 ; Di Paola R4 ; Impellizzeri D4 ; Fusco R4 ; Mercalli V1 ; Massarotti A1 ; Stortini G5 ; Terrazzino S1 Show All Authors
Authors
  1. Travelli C1
  2. Aprile S1
  3. Rahimian R2, 3
  4. Grolla AA1
  5. Rogati F1
  6. Bertolotti M1
  7. Malagnino F1
  8. Di Paola R4
  9. Impellizzeri D4
  10. Fusco R4
  11. Mercalli V1
  12. Massarotti A1
  13. Stortini G5
  14. Terrazzino S1
  15. Del Grosso E1
  16. Fakhfouri G2
  17. Troiani MP6
  18. Alisi MA6
  19. Grosa G1
  20. Sorba G1
  21. Canonico PL1
  22. Orsomando G7
  23. Cuzzocrea S4
  24. Genazzani AA1
  25. Galli U1
  26. Tron GC1
Show Affiliations
Authors Affiliations
  1. 1. Dipartimento di Scienze del Farmaco, Universita degli Studi del Piemonte Orientale “A. Avogadro�, Largo Donegani 2, Novara, 28100, Italy
  2. 2. Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Psychiatry and Neuroscience, Faculty of Medicine, Research Center of the Mental Health Institute of Quebec, Laval University, Quebec, G1J 2G3, QC, Canada
  4. 4. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Via C. Valeria Gazzi, Messina, 98100, Italy
  5. 5. Department of Oncology, Nerviano Medical Sciences Srl, Viale Pasteur 10, Nerviano, Milan, 20014, Italy
  6. 6. R&D, Angelini Research Center, Piazzale della Stazione, S. Palomba-Pomezia, 00040, Italy
  7. 7. Department of Clinical Sciences (DISCO), Section of Biochemistry, Polytechnic University of Marche, Via Ranieri 67, Ancona, 60131, Italy

Source: Journal of Medicinal Chemistry Published:2017


Abstract

Nicotinamide phosphoribosyltransferase (NAMPT) is a key enzyme involved in the recycling of nicotinamide to maintain adequate NAD levels inside the cells. It has been postulated to be a pharmacological target, as it is overexpressed in cancer cells as well as in inflammatory diseases. We describe the synthesis and characterization of a novel class of one-digit nanomolar NAMPT inhibitors based on in vitro characterization. The most active compound tested, 30c, displayed activity in xenograft and allograft models, strengthening the potential of NAMPT inhibitors as antitumoral drugs. Furthermore, in the present contribution we describe the ability of 30c to significantly improve the outcome of colitis in mice. Given that this is the first report of an effect of NAMPT inhibitors in colitis, this result paves the way for novel applications for this class of compounds. © 2017 American Chemical Society.
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