Literature DB >> 26384287

Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.

Jang-Sik Choi1, Hae-Jun Hwang2, Se-Won Kim2, Byung Il Lee3, Jaekyoo Lee4, Ho-Juhn Song4, Jong Sung Koh4, Jung-Ho Kim5, Phil Ho Lee6.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

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

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Substances:

Year:  2015        PMID: 26384287     DOI: 10.1016/j.bmcl.2015.09.011

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Crystal Structures of Spleen Tyrosine Kinase in Complex with Two Novel 4-Aminopyrido[4,3-d] Pyrimidine Derivative Inhibitors.

Authors:  Sang Jae Lee; Jang-Sik Choi; Seoung Min Bong; Hae-Jun Hwang; Jaesang Lee; Ho-Juhn Song; Jaekyoo Lee; Jung-Ho Kim; Jong Sung Koh; Byung Il Lee
Journal:  Mol Cells       Date:  2018-06-12       Impact factor: 5.034

  1 in total

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