Document Type
Patent
Publication Date
June 2013
Patent Number
8466157
Abstract
Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl4. The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.
Application Number
13/225,976
Recommended Citation
Lawrence, Harshani; Ge, Yiyu; Sebti, Said M.; and Guida, Wayne, "Proteasome inhibitors having chymotrypsin-like activity" (2013). USF Patents. 223.
https://digitalcommons.usf.edu/usf_patents/223
Assignees
University of South Florida H. Lee Moffitt Cancer Center and Research Institute, Inc.
Filing Date
09/06/2011
Primary/U.S. Class
514/253
