Benzisothiazolones as modulators of macrophage migration inhibitory factor.

Benzisothiazolones as modulators of macrophage migration inhibitory factor.
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DOI:
10.1016/j.bmcl.2011.05.127
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发表时间:
2011-08-01
影响因子:
2.7
通讯作者:
Bucala, Richard
Bucala, Richard
中科院分区:
医学4区
文献类型:
--
作者:
Jorgensen, William L.;Trofimov, Alexander;Du, Xin;Hare, Alissa A.;Leng, Lin;Bucala, Richard

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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. 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.
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