专利号:US-8119653-B2 优先权日:2006-07-07 标 题 :Belactosin derivatives as therapeutic agents/biological probes and their synthesis 发明人:ROMO DANIEL; CHO SUNG WOOK; SMITH JEFFREY W; RICHARDSON ROBYN D 权利人:ROMO DANIEL; CHO SUNG WOOK; SMITH JEFFREY W; RICHARDSON ROBYN D; TEXAS A & M UNIV SYS 摘要: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.
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