University of South Florida

The Hong Kong Polytechnic University

Mcgill University

Wayne State University

Universitá Degli Studi Di Padova

Centro Di Riferimento Oncologico

Q Ping Dou

David M Smith

Tak-Hang Chan

Edward Turos

Fernando Formaggio

Dolores Fregona

Luca Ronconi

Donatella Aldinucci

Sangkil Nam

The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.

Polyphenol proteasome inhibitors, synthesis, and methods of use

The invention concerns Au(III) complexes of the type [AuX(Pdtc)] (X=halogen, pseudo-halogen; pdtc=peptide-/esterified peptidedithiocarbamato) which are able to both maintain the antitumor properties and the lack of nephrotoxic side-effects of the previously reported Au(III)-dithiocarbamato complexes, together with an improved bioavailability through the peptide-mediated cellular internalization. The Au(III) complexes described have shown a significant biological activity on human tumor cell lines and, thus, they can be advantageously used as antineoplastic agents. The preparation method and use for the treatment of tumor pathologies of the Au(III) complexes of the invention are further described.

Gold (III) complexes with oligopeptides functionalized with sulfur donors and use thereof as antitumor agents

The subject invention concerns N-thiolated &#x3b2;-lactam compounds of formula A, wherein Ris a hydrocarbon group having 1-8 carbon atoms; Ris an organothio group; and Ris alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, and analogs and pharmaceutically acceptable salts, esters and amides thereof. The subject invention also concerns methods for inducing tumor cell death or inhibiting tumor cell proliferation, and methods for inducing DNA damage, inhibiting DNA replication, activating p38 MAP kinase, or activating caspase cascade activation, or releasing cytochrome C from mitochondria into the cytoplasm in a tumor cell. Methods for treating cancer using N-thiolated &#x3b2;-lactam compounds, as well as pharmaceutical compositions comprising the same are further disclosed.

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The subject invention concerns N-thiolated &#x3b2;-lactam compounds of formula A,wherein Ris a hydrocarbon group having 1&#x2013;8 carbon atoms; Ris an organothio group; and Ris alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, and analogs and pharmaceutically acceptable salts, esters and amides thereof. The subject invention also concerns methods for inducing tumor cell death or inhibiting tumor cell proliferation, and methods for inducing DNA damage, inhibiting DNA replication, activating p38 MAP kinase, or activating caspase cascade activation, or releasing cytochrome C from mitochondria into the cytoplasm in a tumor cell. Methods for treating cancer using N-thiolated &#x3b2;-lactam compounds, as well as pharmaceutical compositions comprising the same are further disclosed.

Methods for preventing and treating cancer using N-thiolated &#x3b2;-lactam compounds and analogs thereof

Disclosed herein are ester-bond containing tea polyphenols that has a susceptibility to nucleophilic attack, their analogs and pharmaceutically acceptable salts, method for inhibiting proteasomal chymotrypsin-like activity in vivo and in vitro, methods for cancer treatment with tea-derived polyphenols, such as EGCG, ECG, GCG, or CG, as well as pharmaceutical compositions comprising the same.

Tea polyphenol esters and analogs thereof for cancer prevention and treatment

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Grosse Pointe, MI, United States of America

Q Ping Dou