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Induction of apoptosis by beta-diketones in human tumor cells.

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A variety of beta-diketones were evaluated for their cytotoxic profiles against oral human normal and tumor cells. Among 22 compounds (BD1-22) tested, the cytotoxicity of 3-formylchromone (BD17) (CC50=7.8 microg/mL) against human oral squamous cell carcinoma (HSC-2) cells was higher than that of

Inhibitory effects of 1,3-bis-(2-substituted-phenyl)-propane-1,3-dione, β-diketone structural analogues of curcumin, on chemical-induced tumor promotion and inflammation in mouse skin.

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Dibenzoylmethane (DBM), a β-diketone structural analogue of curcumin, has been reported to exhibit anti-tumorigenic and chemopreventive activities. Due to the structural resemblance of DBM to the anti-inflammatory curcumin and an aspirin-like skeleton of DBM derivatives, we tested the

Effect of the beta-diketones diferuloylmethane (curcumin) and dibenzoylmethane on rat mammary DNA adducts and tumors induced by 7,12-dimethylbenz[a]anthracene.

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Curcumin is a beta-diketone constituent of the spice turmeric that possesses anticarcinogenic properties in several animal models. The present studies were conducted in order to identify beta-diketones structurally-related to curcumin that would be effective dietary blocking agents toward the

Antitumor effects of curcumin and structurally beta-diketone modified analogs on multidrug resistant cancer cells.

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Using concepts of bioisostery a series of curcumin analogs were synthesized: the diketonic system of the compound was elaborated into enaminones, oximes, and the isoxazole heterocycle. The cell growth inhibitory and apoptosis inducing effects of the new analogs were evaluated by in vitro assays in

Heterocyclic cyclohexanone monocarbonyl analogs of curcumin can inhibit the activity of ATP-binding cassette transporters in cancer multidrug resistance.

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Curcumin (CUR) is a phytochemical that inhibits the xenobiotic ABC efflux transporters implicated in cancer multidrug resistance (MDR), such as P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and multidrug resistance-associated proteins 1 and 5 (MRP1 and MRP5). The use of CUR in the

Curcumin: A Potent Modulator of Multiple Enzymes in Multiple Cancers.

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Curcumin (diferuloylmethane) is the biphenolic active compound of turmeric. Curcumin has been used for hundreds of years to treat various ailments. Curcumin has been reported to exert numerous pharmacological effects by modulating multiple molecular targets including those involved in the

Antitumor agents. 217. Curcumin analogues as novel androgen receptor antagonists with potential as anti-prostate cancer agents.

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A number of curcumin analogues were prepared and evaluated as potential androgen receptor antagonists against two human prostate cancer cell lines, PC-3 and DU-145, in the presence of androgen receptor (AR) and androgen receptor coactivator, ARA70. Compounds 4

Design, synthesis and in vitro cell-based evaluation of the anti-cancer activities of hispolon analogs.

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Phytochemicals play an important role in cancer therapy. Hispolon and 26 of its analogs (9 known and 17 new) were synthesized and evaluated for their antiproliferative activities in a panel of six independent human cancer cell lines using the in vitro cell-based MTT assay. Among the hispolon analogs

Cytotoxicity of a series of ferrocene-containing beta-diketones.

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BACKGROUND Oxidised ferrocenium compounds often possess antineoplastic activity. In contrast, reduced ferrocene derivatives frequently only show activity if cell components can oxidise them inside cells to the ferrocenium species. Ferrocene compounds having the lowest formal reduction potential are

Cytotoxicity of ruthenocene-containing β-diketones.

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BACKGROUND Ferrocene-containing β-diketones and cisplatin, [(NH(3))(2)PtCl(2)], possess strong antineoplastic activity. No information is available regarding the anticancer activity of the corresponding ruthenocene complexes. This study examined the cytotoxicity of stable ruthenocene-containing

Dibenzoylmethane induces cell cycle deregulation in human prostate cancer cells.

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Dibenzoylmethane (DBM), a minor beta-diketone constituent of licorice and sunscreens, has been shown to exhibit anti-neoplastic effects in chemically induced skin and mammary cancers in several animal models. To date, no mechanism for the growth inhibitory effects of DBM on prostate cancer cells has

Dietary feeding of dibenzoylmethane inhibits prostate cancer in transgenic adenocarcinoma of the mouse prostate model.

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Dibenzoylmethane (DBM), a minor beta-diketone constituent of licorice, has been shown to exhibit antineoplastic effects in prostate cancer cell lines by induction of cell cycle arrest and regulation of androgen receptor expression. In the present study, we investigated the in vitro and in vivo

Design, synthesis and cytotoxic effects of curcuminoids on HeLa, K562, MCF-7 and MDA-MB-231 cancer cell lines.

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BACKGROUND Curcumin is one of the leading compound extracted from the dry powder of Curcuma longa (Zingiberaceae family), which possess several pharmacological properties. However, in vivo administration exhibited limited applications in cancer therapies. RESULTS Twenty-four curcumin derivatives

A novel curcumin analog (H-4073) enhances the therapeutic efficacy of cisplatin treatment in head and neck cancer.

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Chemotherapy constitutes the standard modality of treatment for localized head and neck squamous cell carcinomas (HNSCC). However, many patients fail to respond and relapse after this treatments due to the acquisition of chemo-resistance. Therefore, there is an urgent need to develop novel drugs

Modulation of arachidonic acid metabolism by curcumin and related beta-diketone derivatives: effects on cytosolic phospholipase A(2), cyclooxygenases and 5-lipoxygenase.

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Aberrant arachidonic acid metabolism is involved in the inflammatory and carcinogenic processes. In this study, we investigated the effects of curcumin, a naturally occurring chemopreventive agent, and related beta-diketone derivatives on the release of arachidonic acid and its metabolites in the

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