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A new class of flavonol-based anti-prostate cancer agents: Design, synthesis, and evaluation in cell models.

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Flavonoids are a large class of polyphenolic compounds ubiquitously distributed in dietary plants with an array of biological activities. Flavonols are a major sub-class of flavonoids featuring a hydroxyl group at C-3. Certain natural flavonols, such as quercetin and fisetin, have been shown by in

Flavones and flavonols may have clinical potential as CK2 inhibitors in cancer therapy.

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The serine-threonine kinase CK2, which targets over 300 cellular proteins, is overexpressed in all cancers, presumably reflecting its ability to promote proliferation, spread, and survival through a wide range of complementary mechanisms. Via an activating phosphorylation of Cdc373, a co-chaperone

Synergistic antiproliferative action of the flavonols quercetin and kaempferol in cultured human cancer cell lines.

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The consumption of vegetables containing the flavonols quercetin and kaempferol reduces the risk of cancer. We utilized human gut (HuTu-80 and Caco-2) and breast cancer cells (PMC42) to show the synergistic effect of quercetin and kaempferol in reducing cell proliferation. A trend in reduction of

Dietary flavonols contribute to false-positive elevation of homovanillic acid, a marker of catecholamine-secreting tumors.

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BACKGROUND Urinary homovanillic acid (HVA) measurement is used routinely as a marker of the first test for the screening of catecholamine-secreting tumors and dopamine metabolism, but generates a large number of false-positive results. With no guidelines for dietary restrictions prior to the test,

Correlations between urinary concentrations and dietary intakes of flavonols in the European Prospective Investigation into Cancer and Nutrition (EPIC) study.

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In this study, we aimed to study the correlation between acute and habitual intakes of flavonols, their main food sources and their 24-h urinary concentrations in an European population.A 24-h dietary recall (24-HDR) and 24-h urine samples were collected on

A food pattern that is predictive of flavonol intake and risk of pancreatic cancer.

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BACKGROUND In the Multiethnic Cohort (MEC) study, we showed inverse associations between flavonols and pancreatic cancer risk. OBJECTIVE We aimed to define a food pattern associated with intakes of quercetin, kaempferol, and myricetin; to examine the association of that pattern with pancreatic

Anti-androgenic effects of flavonols in prostate cancer.

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Dietary-derived agents, such as the flavonoids, are of particular interest for prostate cancer (PCa) chemoprevention as they may offer a favourable safety and side-effect profile. An agent that demonstrates action on the androgen receptor (AR) axis may have value for preventing or treating

Synthesis and biological evaluation of novel flavonols as potential anti-prostate cancer agents.

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A library of flavonol analogues was synthesised and evaluated as potential anticancer agents against a human prostate cancer cell line, 22rν1. Compounds 3, 8 and 11 (IC(50) 2.6, 3.3 and 4.0 μM respectively) showed potent cancer cell growth inhibition, comparable to the lead compound

In vitro activity of dietary flavonol congeners against human cancer cell lines.

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BACKGROUND Flavonoids have physiological activity and a variety of pharmacological properties, including anticancer activity in vitro, but structure-anticancer activity relationships are unclear. OBJECTIVE The objectives of this work were to investigate the activity of dietary flavonol congeners

Tea flavonols in cardiovascular disease and cancer epidemiology.

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Tea is an important dietary source of flavonols in countries such as the Netherlands, the United Kingdom and Japan. Flavonols may have beneficial health effects because of their antioxidant properties and their inhibitory role in various stages of tumor development in animal studies. The association

Dietary flavonols and flavonol-rich foods intake and the risk of breast cancer.

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Laboratory and animal studies suggest that dietary flavonols may reduce breast cancer risk but there are limited epidemiological studies. We computed flavonol intakes from dietary data collected by validated food frequency questionnaires in 1991 and 1995 from 90,630 women in the Nurses Health Study

Flavonol regulation in tumor cells.

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Flavonols comprise a group of flavonoid molecules that are widely distributes in fruits and vegetables. There is epidemiological data to suggest that consumption of flavonols can be accompanied by decreased cancer incidence. The anti-oxidant activity of flavonols may have an important role in

Preferential targeting cancer-related i-motif DNAs by the plant flavonol fisetin for theranostics applications.

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The relationship of i-motif DNAs with cancer has prompted the development of specific ligands to detect and regulate their formation. Some plant flavonols show unique fluorescence and anti-cancer properties, which suggest the utility of the theranostics approach to cancer therapy related to i-motif

Chrysosplenol d, a Flavonol from Artemisia annua, Induces ERK1/2-Mediated Apoptosis in Triple Negative Human Breast Cancer Cells

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Triple negative human breast cancer (TNBC) is an aggressive cancer subtype with poor prognosis. Besides the better-known artemisinin, Artemisia annua L. contains numerous active compounds not well-studied yet. High-performance liquid chromatography coupled with diode-array and mass

The dietary flavonol fisetin enhances the apoptosis-inducing potential of TRAIL in prostate cancer cells.

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Tumour necrosis factor-related apoptosis-inducing ligand (TRAIL) is an endogenous agent that induces apoptosis selectively in cancer cells. Soluble or expressed in immune cells, TRAIL plays an important role in the defense against tumour cells. The resistance of cancer cells to TRAIL immune

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