Invention Grant
US08193377B2 (−)-epigallocatechin gallate derivatives for inhibiting proteasome
有权
( - ) - 表没食子儿茶素没食子酸酯衍生物用于抑制蛋白酶体
- Patent Title: (−)-epigallocatechin gallate derivatives for inhibiting proteasome
- Patent Title (中): ( - ) - 表没食子儿茶素没食子酸酯衍生物用于抑制蛋白酶体
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Application No.: US11660513Application Date: 2005-08-15
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Publication No.: US08193377B2Publication Date: 2012-06-05
- Inventor: Tak-Hang Chan , Wai-Har Lam , Larry Ming-Cheung Chow , Qing Ping Dou , Deborah Joyce Kuhn , Aslamuzzaman Kazi , Sheng Biao Wan , Kristin R. Landis-Piwowar
- Applicant: Tak-Hang Chan , Wai-Har Lam , Larry Ming-Cheung Chow , Qing Ping Dou , Deborah Joyce Kuhn , Aslamuzzaman Kazi , Sheng Biao Wan , Kristin R. Landis-Piwowar
- Applicant Address: HK Hung Hom, Kowloon US MI Detroit US FL Tampa
- Assignee: The Hong Kong Polytechnic University,Wayne State University,University of South Florida
- Current Assignee: The Hong Kong Polytechnic University,Wayne State University,University of South Florida
- Current Assignee Address: HK Hung Hom, Kowloon US MI Detroit US FL Tampa
- Agency: Buchanan Ingersoll & Rooney PC
- International Application: PCT/CN2005/001262 WO 20050815
- International Announcement: WO2006/017981 WO 20060223
- Main IPC: C07D311/00
- IPC: C07D311/00 ; A01N43/16

Abstract:
(−)-EGCG, the most abundant catechin, was found to be chemopreventive and anticancer agent. However, (−)-EGCG has at least one limitation: it gives poor bioavailability. This invention provides compounds of generally formulae below, wherein R11, R12, R13, R21, R22, R2, R3, and R4 are each independently selected from the group consisting of —H, and C1 to C10 acyloxyl group; and R5 is selected from the group consisting of —H, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl and C3-C7-cycloalkenyl, whereas each of the last mentioned 7 groups can be substituted with any combination of one to six halogen atoms; at least one of R11, R12, R13, R21, R22, R2, R3 and R4 is —H, which were found to be more potent than their non-protected counterparts, which can be used as proteasome inhibitors to reduce tumor cell growth.
Public/Granted literature
- US20080176931A1 (-)-Epigallocatechin Gallate Derivatives For Inhibiting Proteasome Public/Granted day:2008-07-24
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