727664-90-6Relevant academic research and scientific papers
Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1
Bravo, Yalda,Teriete, Peter,Dhanya, Raveendra-Panickar,Dahl, Russell,Lee, Pooi San,Kiffer-Moreira, Tina,Ganji, Santhi Reddy,Sergienko, Eduard,Smith, Layton H.,Farquharson, Colin,Millan, Jose Luis,Cosford, Nicholas D.P.
, p. 4308 - 4311 (2014/09/17)
We report the discovery and characterization of a series of benzoisothiazolone inhibitors of PHOSPHO1, a newly identified soluble phosphatase implicated in skeletal mineralization and soft tissue ossification abnormalities. High-throughput screening (HTS)
Benzisothiazolones as modulators of macrophage migration inhibitory factor
Jorgensen, William L.,Trofimov, Alexander,Du, Xin,Hare, Alissa A.,Leng, Lin,Bucala, Richard
, p. 4545 - 4549 (2011/09/12)
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.
