Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).

Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).

Bioorganic & medicinal chemistry letters (2008-10-22)

Luc J Farmer, Guy Bemis, Shawn D Britt, John Cochran, Martin Connors, Edmund M Harrington, Thomas Hoock, William Markland, Suganthini Nanthakumar, Paul Taslimi, Ernst Ter Haar, Jian Wang, Darshana Zhaveri, Francesco G Salituro

PMID18938080

RÉSUMÉ

A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead 4 were prepared and evaluated for biological activity. Lead optimization provided compounds with nanomolar K(i)'s against SYK and potent inhibition in mast cell degranulation assays.