(−)-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.
Chan, Tak-Hang; Lam, Wai-Har; Chow, Larry Ming-Cheung; Dou, Qing Ping; Kuhn, Deborah Joyce; and Kazi, Aslamuzzaman, "(−)-Epigallocatechin gallate derivatives for inhibiting proteasome" (2009). USF Patents. 559.
The Hong Kong Polytechnic University