发明名称 (-)-Epigallocatechin gallate derivatives for inhibiting proteasome
摘要 (-)-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 formula 10, wherein R1 is selected from the group of -H and C1 to C6 acyl group; R2, R3, and R4 are each independently selected from the group of -H, -OH, and C1 to C6 acyloxyl group; and at least one of R2, R3, or R4 is -H. The derivatives of (-)-EGCG that is at least as potent as (-)-EGCG. The carboxylate protected forms of (-)-EGCG and its derivatives are found to be more stable than the unprotected forms, which can be used as proteasome inhibitors to reduce tumor cell growth.
申请公布号 US7544816(B2) 申请公布日期 2009.06.09
申请号 US20040921332 申请日期 2004.08.19
申请人 THE HONG KONG POLYTECHNIC UNIVERSITY;WAYNE STATE UNIVERSITY;UNIVERSITY OF SOUTH FLORIDA;MCGILL UNIVERSITY 发明人 CHAN TAK-HANG;LAM WAI-HAR;CHOW LARRY MING-CHEUNG;DOU QING PING;KUHN DEBORAH JOYCE;KAZI ASLAMUZZAMAN
分类号 C07D311/82;A61K31/35 主分类号 C07D311/82
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