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Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders.
- Maria Gabriella Brasca, Paola Gnocchi, Marcella Nesi, Nadia Amboldi, Nilla Avanzi, Jay Bertrand, Simona Bindi, Giulia Canevari, Daniele Casero, Marina Ciomei, Nicoletta Colombo, Sabrina Cribioli, Gabriele Fachin, Eduard R Felder, Arturo Galvani, Antonella Isacchi, Ilaria Motto, Achille Panzeri, 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. 2015 May 15; 23 (10): 2387-407.
AbstractCompound 1, a hit from the screening of our chemical collection displaying activity against JAK2, was deconstructed for SAR analysis into three regions, which were explored. A series of compounds was synthesized leading to the identification of the potent and orally bioavailable JAK2 inhibitor 16 (NMS-P830), which showed an encouraging tumour growth inhibition in SET-2 xenograft tumour model, with evidence for JAK2 pathway suppression demonstrated by in vivo pharmacodynamic effects. Copyright © 2015 Elsevier Ltd. All rights reserved.
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