Belactosin derivatives as therapeutic agents/biological probes and their synthesis
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Derivatives of belactosin and their synthesis are disclosed. In certain embodiments, compounds of the present invention exhibit anti-cancer, antiviral, antibiotic, and/or auto-immune therapeutic abilities. In general, methods of synthesis disclosed herein allow for introduction of a variety of substituents at numerous positions as well as the facile introduction of a beta-lactone ring moiety. The synthetic steps comprise, in preferred embodiments, a tandem Mukaiyama aldol lactonization reaction. Data demonstrating the utility of some of the derivatives as proteasome inhibitors is also disclosed.
Romo, Daniel; Cho, Sung Wook; Smith, Jeffrey W.; Richardson, Robyn D. (2012). Belactosin derivatives as therapeutic agents/biological probes and their synthesis. United States. Patent and Trademark Office; Texas A&M University. Libraries. Available electronically from