(−)-Epigallocatechin gallate derivatives for...

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S456000

Reexamination Certificate

active

07544816

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 formula 10, wherein R1is selected from the group of —H and C1to C6acyl group; R2, R3, and R4are each independently selected from the group of —H, —OH, and C1to C6acyloxyl group; and at least one of R2, R3, or R4is —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.

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