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ID: ALA1130806
Journal: Bioorg Med Chem Lett
Title: Enhanced potency of perfluorinated thalidomide derivatives for inhibition of LPS-induced tumor necrosis factor-alpha production is associated with a change of mechanism of action.
Authors: Niwayama S, Loh C, Turk BE, Liu JO, Miyachi H, Hashimoto Y.
Abstract: Perfluorination of phthalimides leads to dramatically increased potency as inhibitors of TNF-alpha production. We examined the enantiodependence for several tetrafluorophthalimides and alpha-methylthalidomide, 3. Only 3 exhibited strikingly enantiodependent activity. The key structural determinant for the enhanced activity is the tetrafluorophthaloyl group, which confers enhanced potency and a change in the mechanism of inhibition.
CiteXplore: 9871710