1.
Bioorg Med Chem Lett
; 21(20): 6188-94, 2011 Oct 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21903390
RESUMO
The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over liability kinases and hERG activity. GSK143 is a potent and highly selective SYK inhibitor showing good efficacy in the rat Arthus model.