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J Med Chem. 2017 Mar 9;60(5):1768-1792. doi: 10.1021/acs.jmedchem.6b01392. Epub 2017 Feb 22.

Identification of Novel Triazole-Based Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors Endowed with Antiproliferative and Antiinflammatory Activity.

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Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale "A. Avogadro" , Largo Donegani 2, 28100 Novara, Italy.
Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences , Tehran, Iran.
Department of Psychiatry and Neuroscience, Faculty of Medicine, Research Center of the Mental Health Institute of Quebec, Laval University , Quebec, Quebec G1J 2G3, Canada.
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina , Via C. Valeria Gazzi, 98100 Messina, Italy.
Department of Oncology, Nerviano Medical Sciences Srl , Viale Pasteur 10, 20014 Nerviano, Milan, Italy.
R&D, Angelini Research Center, Piazzale della Stazione, 00040 S. Palomba-Pomezia, Italy.
Department of Clinical Sciences (DISCO), Section of Biochemistry, Polytechnic University of Marche , Via Ranieri 67, 60131 Ancona, Italy.


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.

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