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

DOI: 10.1016/j.bmcl.2008.09.106

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 6231 - 6235 (2008)

Update date:2022-09-26

Topics:

Authors:

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.

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Article abstract of DOI:10.1016/j.bmcl.2008.09.106

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.

Full text of DOI:10.1016/j.bmcl.2008.09.106

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