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ID: ALA2069193

Journal: Bioorg Med Chem Lett

Title: Highly potent aminopyridines as Syk kinase inhibitors.

Authors: Castillo M, Forns P, Erra M, Mir M, López M, Maldonado M, Orellana A, Carreño C, Ramis I, Miralpeix M, Vidal B.

Abstract: A novel class of potent Syk inhibitors has been developed from rational design. Highly potent aminopyridine derivatives bearing a 4-trifluoromethyl-2-pyridyl motif and represented by compound 13b IC(50): 0.6 nM were identified. Substitution by a 2-pyrazinyl motif and SAR expansion in position 4 of the central core provided diverse potent non-cytotoxic Syk inhibitors showing nanomolar activity inhibiting human mast cell line LAD2 degranulation.

CiteXplore: 22877633

DOI: 10.1016/j.bmcl.2012.07.045