Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2008 Dec 1;18(23):6231-5. doi: 10.1016/j.bmcl.2008.09.106. Epub 2008 Oct 7.

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

Author information

1
Department of Medicinal Chemistry, Vertex Pharmaceuticals, Inc., 130 Waverly Street, Cambridge, MA 02139, USA. luc_farmer@vrtx.com

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.

PMID:
18938080
DOI:
10.1016/j.bmcl.2008.09.106
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center