In one aspect, the present disclosure provides caffeic acid derivatives of the formula: ##STR00001## wherein the variables are as defined herein. In another aspect, the present disclosure provides pharmaceutical compositions and methods of using of the compounds disclosed herein, including for the treatment of cancer.

Board of Regents, The University of Texas System

Caffeic acid derivatives and uses thereof

The present invention is drawn to the inhibition of activation of NF-.kappa.B by caffeic acid phenethyl ester (CAPE) and two analogues of CAPE. Tumor necrosis factor (TNF) activation of NF-.kappa.B is completely blocked by CAPE in a dose- and time-dependent manner, as is activation by phorbol ester, ceramide, hydrogen peroxide, and okadaic acid. Additionally, capsaicin (8-methyl-N-vanillyl-6-noneamide) and resiniferatoxin inhibit the activation of NF-.kappa.B induced by different agents.

Research Development Foundation

Inhibition of nuclear transcription factor NF-.kappa.B by caffeic acid phenethyl ester (CAPE), derivatives of CAPE, capsaicin (8-methyl-N-vanillyl-6-nonenamide) and resiniferatoxin

A method of inhibiting the formation of a cataract in an eye by contacting the eye with a compound having the structure: ##STR1## is described. Also described is a method of inhibiting the progression of cataract formation in an eye. Methods comprising administering a pharmaceutical composition comprising the above compound to inhibit the formation of a cataract in the eye of a subject and to inhibit progression of cataract formation in the eye of a subject are also described. The above compound also prevents diseases resulting from oxidative stress, including diseases comprising tumor formation resulting from oxidative stress, and also inhibits the progression of diseases resulting from oxidative stress. The above compound may furthermore be used to treat an HIV infection when combined in a pharmaceutical composition with a substance which inhibits HIV replication.

The Trustees of Columbia University in the City of New York

New York University

Inhibition of cataract formation, diseases resulting from oxidative stress, and HIV replication by caffeic acid esters

The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as inhibitors of Jak2/STAT3 pathways and downstream targets and inhibit the growth and survival of cancerous cell lines.

caffeic acid/càncer

Caffeic acid derivatives and uses thereof

Inhibition of nuclear transcription factor NF-.kappa.B by caffeic acid phenethyl ester (CAPE), derivatives of CAPE, capsaicin (8-methyl-N-vanillyl-6-nonenamide) and resiniferatoxin

Inhibition of cataract formation, diseases resulting from oxidative stress, and HIV replication by caffeic acid esters

Orally bioavailable caffeic acid related anticancer drugs

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