Highly potent aminopyridines as Syk kinase inhibitors

…, M López, M Maldonado, A Orellana, C Carreño…

文献索引：Castillo, Marcos; Forns, Pilar; Erra, Montse; Mir, Marta; Lopez, Manel; Maldonado, Monica; Orellana, Adelina; Carreno, Cristina; Ramis, Isabel; Miralpeix, Montserrat; Vidal, Bernat Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 17 p. 5419 - 5423

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被引用次数: 14

摘要

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 IC50: 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.