| Literature DB >> 25882525 |
Maria Gabriella Brasca1, Paola Gnocchi2, Marcella Nesi2, Nadia Amboldi2, Nilla Avanzi2, Jay Bertrand2, Simona Bindi2, Giulia Canevari2, Daniele Casero2, Marina Ciomei2, Nicoletta Colombo2, Sabrina Cribioli2, Gabriele Fachin2, Eduard R Felder2, Arturo Galvani2, Antonella Isacchi2, Ilaria Motto2, Achille Panzeri2, Daniele Donati2.
Abstract
Compound 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.Entities:
Keywords: Anti-cancer agents; JAK2; Myeloproliferative disorders; Protein kinase inhibitor; Tumour cell proliferation inhibition
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Year: 2015 PMID： 25882525 DOI： 10.1016/j.bmc.2015.03.059
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641