1056476-98-2Relevant academic research and scientific papers
Isosteric exchange of the acylsulfonamide moiety in Abbott's Bcl-XL protein interaction antagonist
Doemling, Alexander,Antuch, Walfrido,Beck, Barbara,Schauer-Vukasinovic, Vesna
, p. 4115 - 4117 (2008)
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.
