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Isosteric exchange of the acylsulfonamide moiety in Abbott's Bcl-XL protein interaction antagonist. | LitMetric

AI Article Synopsis

Article 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.

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http://dx.doi.org/10.1016/j.bmcl.2008.05.096DOI Listing

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