The Hong Kong Polytechnic University

University of South Florida

Wayne State University

Mcgill University

Larry Ming-Cheung Chow

Tak-Hang Chan

Deborah Joyce Kuhn

Qing Ping Dou

Aslamuzzaman Kazi

Wai-Har Lam

Iris Lai King Wong

Kin-Fai Chan

Sheng Biao Wan

Kristin R Landis-Piwowar

Wing-Yiu Kan

Tak Hang William Chan

William Tak Hang Chan

The present invention relates to novel series of amine-containing flavonoids and compositions containing the compounds, as well as the synthesis and the use of the same. The invention also relates to methods of treatment and prevention of diseases, in particular, parasitic infections including Leishmaniasis, comprising administration of the compounds.

Synthesis and use of amine-containing flavonoids as potent anti-leishmanial agents

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

This invention relates to bis-flavonoid compounds, their synthesis and use for inhibiting multidrug resistance in chemotherapy and protozoan infection, wherein the bis-flavonoids compounds have the formula: 

Flavonoid dimers and their use

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

Multidrug resistance (MDR) is a major problem in cancer chemotherapy. The best characterized resistance mechanism is the one mediated by the over-expression of drug efflux transporters, permeability-glycoprotein (P-gp), which pump a variety of anticancer drugs out of the cells, resulting in lowered intracellular drug accumulation. A series of flavonoid dimers are developed in this invention, which are linked together by linker groups of various lengths. These flavonoid dimers are found to be efficient P-gp modulators that increase cytotoxicity of anticancer drugs in vitro and dramatically enhance their intracellular drug accumulation. It is found that the flavonoid dimers of this invention is also useful in reducing drug resistance in treating parasitic diseases.

Flavonoid dimers and methods of making and using such

(&#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. 

Growing community of inventors

Hong Kong, China

Larry Ming-Cheung Chow