Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594558 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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 IC50: 0.6Â 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.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Marcos Castillo, Pilar Forns, Montse Erra, Marta Mir, Manel López, Mónica Maldonado, Adelina Orellana, Cristina Carreño, Isabel Ramis, Montserrat Miralpeix, Bernat Vidal,