Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.

Bioorganic & medicinal chemistry letters ·Vol. 25 ·No. 20 ·2016-04-20

Choi Jang-Sik, Hwang Hae-Jun, Kim Se-Won, Lee Byung Il, Lee Jaekyoo, Song Ho-Juhn, Koh Jong Sung, Kim Jung-Ho, Lee Phil Ho

Abstract

A series of pyrazolylpyrimidine scaffold based Syk inhibitors were synthesized and evaluated for their biological activities and selectivity. Lead optimization efforts provided compounds with potent Syk inhibition in both enzymatic and TNF-α release assay.

Keywords

Pyrazolylpyrimidine Rheumatoid arthritis Spleen tyrosine kinase Structure–activity relationship Syk inhibitors

Article Info

Journal

Bioorganic & medicinal chemistry letters

Abbr.

Bioorg Med Chem Lett

ISSN

0960-894X

DOI

10.1016/j.bmcl.2015.09.011

Published

2016-04-20

Indexed

2015-10-03

Updated

2016-11-25

Language

English

Country/Region

England

NLM ID

9107377

External Links

PubMed source DOI: 10.1016/j.bmcl.2015.09.011 View journal details

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Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.

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