Polyphenol proteasome inhibitors, synthesis, and methods of use (Divisional)

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.

Inventor: Dou, Q. Ping | Chan, Tak-Hang | Smith, David M.
Priority Number: US8058310B2
IPC Current: A61K0031235 | A61K003116 | C07C006988 | C07C023554 | C07D031160
US Class: 514543 | 514616
Assignee Applicant: University of South Florida,Tampa | McGill University | The Hong Kong Polytechnic University
Title: Polyphenol proteasome inhibitors, synthesis, and methods of use
Usefulness: Polyphenol proteasome inhibitors, synthesis, and methods of use
Summary: (I) are useful for: treating cancer consisting of prostate cancer, leukemia, hormone dependent cancers, breast cancer, colon cancer, lung cancer, epidermal cancer, liver cancer, esophageal cancer, stomach cancer, cancer of the brain, and cancer of the kidney; increasing the relative proportion of cells occupying the G1 phase of the mitotic cell cycle within the cells; and inducing apoptosis in many cells (cancer cells) (all claimed).
Novelty: New e.g. substituted N-(2-phenyl-chroman-3-yl)-benzamide compounds and trihydroxybenzoyl-oxycyclohexyl-3,4,5-trihydroxybenzoate are 20S proteasome inhibitors, useful to treat e.g. prostate cancer and leukemia

Disease Diagnostic/Treatment

Cancer/Tumor

Chan T.H.
SMITH D.M.(South Florida Uni)
DOU Q. Ping (South Florida Uni)

USA