| Literature DB >> 21719283 |
William L Jorgensen1, Alexander Trofimov, Xin Du, Alissa A Hare, Lin Leng, Richard Bucala.
Abstract
Substituted N-phenylbenzisothiazolones have been investigated as inhibitors of the tautomerase activity of the proinflammatory cytokine MIF (macrophage migration inhibitory factor). Numerous compounds were found to possess antagonist activity in the low micromolar range with the most potent being the 6-hydroxy analog 1w. Compound 1w and the p-cyano analog 1c were also shown to exhibit significant inhibition of the binding of MIF to its transmembrane receptor CD74. Consistently, both compounds were also found to retard the MIF-dependent phosphorylation of ERK1/2 in human synovial fibroblasts.Entities:
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Year: 2011 PMID： 21719283 PMCID： PMC3139435 DOI： 10.1016/j.bmcl.2011.05.127
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823