NOVEL BELACTOSIN DERIVATIVES AS THERAPEUTIC AGENTS/BIOLOGICAL PROBES AND THEIR SYNTHESIS

摘要

Derivatives of belactosin and their synthesis are disclosed. In certain e mbodiments, compounds of the present invention exhibit anti-cancer, antivira l, antibiotic, and/or autoimmune therapeutic abilities. In general, methods of synthesis disclosed herein allow for introduction of a variety of substit uents at numerous positions as well as the facile introduction of a beta-lac tone ring moiety. The synthetic steps comprise, in preferred embodiments, a tandem Mukaiyama aldol lactonization reaction. Data demonstrating the utilit y of some of the derivatives as proteasome inhibitors is also disclosed.