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Bioorg Med Chem Lett. 2011 Aug 1;21(15):4545-9. doi: 10.1016/j.bmcl.2011.05.127. Epub 2011 Jun 12.

Benzisothiazolones as modulators of macrophage migration inhibitory factor.

Author information

1
Department of Chemistry, Yale University, New Haven, CT 06520-8107, USA. william.jorgensen@yale.edu

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.

PMID:
21719283
PMCID:
PMC3139435
DOI:
10.1016/j.bmcl.2011.05.127
[Indexed for MEDLINE]
Free PMC Article

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