• Bioorg. Med. Chem. · Sep 2014

    Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.

    • Maria Gabriella Brasca, Marcella Nesi, Nilla Avanzi, Dario Ballinari, Tiziano Bandiera, Jay Bertrand, Simona Bindi, Giulia Canevari, Davide Carenzi, Daniele Casero, Lucio Ceriani, Marina Ciomei, Alessandra Cirla, Maristella Colombo, Sabrina Cribioli, Cinzia Cristiani, Franco Della Vedova, Gabriele Fachin, Marina Fasolini, Eduard R Felder, Arturo Galvani, Antonella Isacchi, Danilo Mirizzi, Ilaria Motto, Achille Panzeri, Enrico Pesenti, Paola Vianello, Paola Gnocchi, and Daniele Donati.
    • Nerviano Medical Sciences S.r.l., Oncology, Viale Pasteur 10, 20014 Nerviano (MI), Italy. Electronic address: gabriella.brasca@nervianoms.com.
    • Bioorg. Med. Chem. 2014 Sep 1; 22 (17): 4998-5012.

    AbstractWe report herein the discovery, structure guided design, synthesis and biological evaluation of a novel class of JAK2 inhibitors. Optimization of the series led to the identification of the potent and orally bioavailable JAK2 inhibitor 28 (NMS-P953). Compound 28 displayed significant tumour growth inhibition in SET-2 xenograft tumour model, with a mechanism of action confirmed in vivo by typical modulation of known biomarkers, and with a favourable pharmacokinetic and safety profile. Copyright © 2014 Elsevier Ltd. All rights reserved.

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