PROTEASOME INHIBITORS HAVING CHYMOTRYPSIN-LIKE ACTIVITY
摘要
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.
申请公布号
WO2010102286(A2)
申请公布日期
2010.09.10
申请号
WO2010US26531
申请日期
2010.03.08
申请人
H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.;UNIVERSITY OF SOUTH FLORIDA;LAWRENCE, HARSHANI;GE, YIYU;SEBTI, SAID M.;GUIDA, WAYNE
发明人
LAWRENCE, HARSHANI;GE, YIYU;SEBTI, SAID M.;GUIDA, WAYNE