Bioorganic & Medicinal Chemistry Letters 2008-12-01

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

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

Index: Bioorg. Med. Chem. Lett. 18(23) , 6231-5, (2008)

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Abstract

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.