John Liddle,
Francis L Atkinson,
Michael D Barker,
Paul S Carter,
Neil R Curtis,
Rob P Davis,
Clement Douault,
Marion C Dickson,
Dorothy Elwes,
Neil S Garton, [......],
Vipulkumar K Patel,
Alex G S Preston,
Cesar Ramirez-Molina,
Tracy J Shipley,
Philip A Skone, Nick Smithers,
Donald O Somers,
Ann L Walker,
Robert J Watson,
Gordon G Weingarten
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ABSTRACT: 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.
Bioorganic & medicinal chemistry letters 08/2011; 21(20):6188-94. · 2.65 Impact Factor
