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ID: ALA1155094
Journal: Bioorg Med Chem Lett
Title: Isosteric exchange of the acylsulfonamide moiety in Abbott's Bcl-XL protein interaction antagonist.
Authors: Dömling A, Antuch W, Beck B, Schauer-Vukasinović V.
Abstract: A multi-component reaction strategy was used for the fast and efficient synthesis of amide isosteres of known Bcl-2 inhibitors capable of disrupting protein-protein interactions. Ugi reaction and a subsequent nucleophilic aromatic substitution reaction provide a versatile path to libraries of compounds similar to Abbott's acylsulfonamides. Modeling arguments are used to explain the inferior activity of the amide as opposed to the sulfonamide series.
CiteXplore: 18583128