发明申请
- 专利标题: AKT INACTIVATION BY TOCOPHERYL DERIVATIVES
- 专利标题(中): 通过TOCOPHERYL衍生物的AKT灭活
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申请号: US13952032申请日: 2013-07-26
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公开(公告)号: US20140031388A1公开(公告)日: 2014-01-30
- 发明人: Ching-Shih Chen , Dasheng Wang , Samuel K. Kulp
- 申请人: Ching-Shih Chen , Dasheng Wang , Samuel K. Kulp
- 主分类号: C07D311/60
- IPC分类号: C07D311/60 ; C07D405/10 ; C07D493/10 ; C07D215/20 ; C07D327/08
摘要:
Anticancer compounds according to formula I are described herein. wherein R1, R2, R3 and R4 are selected from H, CH3, OH, SH, OCH3, NHR′, halogen, CF3, N-linked pyrrolidine, and SO2NHR′, or any combination thereof; R5 is an alkyl, alkenyl, or alkaryl group including from 4 to 11 carbons, X is selected from CH2, CHOH, C═O, S═O, O═S═O, and an oxetane ring, Y is selected from CH2, O, and NH, and R′ is a H, aryl, or a lower alkyl group, or pharmaceutically acceptable salts thereof. The compounds have been shown to facilitate site-specific dephosphorylation of Akt at Ser-473, thereby inactivating Akt and decreasing dysregulation of Akt signaling that can occur in cancer cells.
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