title: Serendipity in discovery of proteasome inhibitors.
abstract: Among its various catalytic activities, the 'chymotrypsin-like' activity of the proteasome, a large multicatalytic proteinase complex has emerged as the focus of drug discovery efforts in cancer therapy. Herein, a series of first generation (2S, 3R)-2-amino-3-hydroxybutyric acid derived proteasome inhibitors that were discovered serendipitously en route to original goal of generating a series of sterically constrained oxazoline derivatives has been reported.
authors.affiliation: Cephalon Inc., 145 Brandywine Parkway, West Chester, PA 19380, United States.
authors.forename: Derek
authors.initials: D
authors.lastname: Dunn
authors.forename: Mohamed
authors.initials: M
authors.lastname: Iqbal
authors.forename: Jean
authors.initials: J
authors.lastname: Husten
authors.forename: Mark A
authors.initials: MA
authors.lastname: Ator
authors.forename: Sankar
authors.initials: S
authors.lastname: Chatterjee
mesh_terms: D004791:Enzyme Inhibitors / Q000494:pharmacology*; D061988:Proteasome Inhibitors
chemical_list: D004791:Enzyme Inhibitors; D061988:Proteasome Inhibitors