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

…, J Cochran, M Connors, EM Harrington, T Hoock…

Index: Farmer, Luc J.; Bemis, Guy; Britt, Shawn D.; Cochran, John; Connors, Martin; Harrington, Edmund M.; Hoock, Thomas; Markland, William; Nanthakumar, Suganthini; Taslimi, Paul; Haar, Ernst Ter; Wang, Jian; Zhaveri, Darshana; Salituro, Francesco G. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 23 p. 6231 - 6235

Full Text: HTML

Citation Number: 26

Abstract

Download PDF Opens in a new window. Article suggestions will be shown in a dialog on return to ScienceDirect. ... Please enable JavaScript to use all the features on this page. ... 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. ... The synthesis of potent novel ...