Development of Benzenesulfonamide Derivatives as Potent Glutathione Transferase Omega-1 Inhibitors
Xie, Yiyue; TUMMALA, PADMAJA; Oakley, Aaron; Deora, Girdhar Singh; Nakano, Yuji; Rooke, Melissa; Cuellar, Matthew; Strasser, Jessica; Dahlin, Jayme L; Walters, Michael A; Casarotto, Marco; Board, Philip; Baell, Jonathan B
Glutathione transferase omega-1 (GSTO1-1) is an enzyme whose function supports the activation of interleukin (IL)- 1β and IL-18 that are implicated in a variety of inflammatory disease states for which small-molecule inhibitors are sought. The potent reactivity of the active-site cysteine has resulted in reported inhibitors that act by covalent labeling. In this study, structure− activity relationship (SAR) elaboration of the reported GSTO1-1 inhibitor C1-27 was undertaken. Compounds...[Show more]
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|Source:||Journal of Medicinal Chemistry|
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