发明申请
- 专利标题： PROTEASOME INHIBITORS HAVING CHYMOTRYPSIN-LIKE ACTIVITY
- 专利标题（中）： 具有抗氧化活性的活性抑制剂
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申请号： US13225976申请日： 2011-09-06
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公开(公告)号： US20120142917A1公开(公告)日： 2012-06-07
- 发明人: Harshani Lawrence , Yiyu Ge , Said M. Sebti , Wayne Guida
- 申请人： Harshani Lawrence , Yiyu Ge , Said M. Sebti , Wayne Guida
- 申请人地址： US FL Tampa US FL Tampa
- 专利权人： H. Lee Moffitt Cancer Center and Research Institute, Inc.,UNIVERSITY OF SOUTH FLORIDA
- 当前专利权人： H. Lee Moffitt Cancer Center and Research Institute, Inc.,UNIVERSITY OF SOUTH FLORIDA
- 当前专利权人地址： US FL Tampa US FL Tampa
- 主分类号： C07D333/34
- IPC分类号： C07D333/34 ; C07D409/12 ; C07D413/12 ; C07C323/67 ; C07C311/20
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.
公开/授权文献
- US08466157B2 Proteasome inhibitors having chymotrypsin-like activity 公开/授权日：2013-06-18
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