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  • Title: Carprofen analogues as sirtuin inhibitors: enzyme and cellular studies.
    Author: Mellini P, Carafa V, Di Rienzo B, Rotili D, De Vita D, Cirilli R, Gallinella B, Provvisiero DP, Di Maro S, Novellino E, Altucci L, Mai A.
    Journal: ChemMedChem; 2012 Nov; 7(11):1905-8. PubMed ID: 24155041.
    Abstract:
    The best of both: SIRT1/2 inhibitors were developed by combining chemical features of selisistat (SIRT1-selective inhibitor; blue) and carprofen (anti-inflammatory drug; red). The most potent compound (shown) increased acetyl-p53 and acetyl-α-tubulin levels, and induced slight apoptosis at 50 μM in U937 cells, differently from selisistat and carprofen.
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