University of South Florida

Wayne State University

The Hong Kong Polytechnic University

Mcgill University

Qing Ping Dou

Tak-Hang Chan

Larry Ming-Cheung Chow

Wai-Har Lam

Deborah Joyce Kuhn

Aslamuzzaman Kazi

Sheng Biao Wan

Kristin R Landis-Piwowar

A method of reducing tumor cell growth, the method including administering an effective amount of a compound having the formula: 

(&#x2212;)-Epigallocatechin gallate derivatives for inhibiting proteasome

(&#x2212;)-epigallocatechin gallate derivatives for inhibiting proteasome

(&#x2212;)-EGCG, the most abundant catechin, was found to be chemopreventive and anticancer agent. However, (&#x2212;)-EGCG has at least one limitation: it gives poor bioavailability. This invention provides compounds of generally formulae below, wherein R, R, R, R, R, R, R, and Rare each independently selected from the group consisting of &#x2014;H, and Cto Cacyloxyl group; and Ris selected from the group consisting of &#x2014;H, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl, phenyl, benzyl and C-C-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 R, R, R, R, R, R, Rand Ris &#x2014;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. 

(&#x2212;)-EGCG, the most abundant catechin, was found to be chemopreventive and anticancer agent. However, (&#x2212;)-EGCG has at least one limitation: it gives poor bioavailability. This invention provides compounds of generally formula 10, wherein Ris selected from the group of &#x2014;H and Cto Cacyl group; R, R, and Rare each independently selected from the group of &#x2014;H, &#x2014;OH, and Cto Cacyloxyl group; and at least one of R, R, or Ris &#x2014;H. The derivatives of (&#x2212;)-EGCG that is at least as potent as (&#x2212;)-EGCG. The carboxylate protected forms of (&#x2212;)-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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Detroit, MI, United States of America

Qing Ping Dou