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Nuclear type-ii [h-3] estradiol binding-sites in mcf-7 human breast-cancer cells - binding interactions with 2,6-bis-([3,4-dihydroxyphenyl]-methylene)cyclohexanone esters and inhibition of cell-proliferation.

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Previous studies from this laboratory demonstrated that 2,6-bis-([3,4-dihydroxyphenyl]methylene)cyclohexanone (BDHPC) and related compounds mimic methyl p-hydroxyphenyllactate (MeHPLA) as endogenous ligands for nuclear type II [H-3]estradiol binding sites. Occupancy of type II sites by these agents

The Molecular Targets and Anti-Invasive Effects of 2,6-bis-(4-hydroxyl-3methoxybenzylidine) cyclohexanone or BHMC in MDA-MB-231 Human Breast Cancer Cells.

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In order to metastasize, tumor cells need to migrate and invade the surrounding tissues. It is important to identify compound(s) capable of disrupting the metastasis of invasive cancer cells, especially for hindering invadopodia formation, so as to provide anti-metastasis targeted therapy.

Mechanisms for the activity of heterocyclic cyclohexanone curcumin derivatives in estrogen receptor negative human breast cancer cell lines.

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Estrogen receptor (ER)-negative breast cancer is an aggressive form that currently requires more drug treatment options. Thus, we have further modified cyclohexanone derivatives of curcumin and examined them for cytotoxicity towards ER-negative human breast cancer cells. Two of the analogs screened

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

A novel curcumin derivative increases the cytotoxicity of raloxifene in estrogen receptor-negative breast cancer cell lines.

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There is a need for new, safe and efficacious drug therapies for the treatment of estrogen receptor (ER)-negative breast cancers. Raloxifene and the 2nd generation curcumin derivative 2,6-bis(pyridin-4-ylmethylene)-cyclohexanone (RL91) have been shown to inhibit the growth of ER-negative breast

Identification of cyclohexanone derivatives that act as catalytic inhibitors of topoisomerase I: effects on tamoxifen-resistant MCF-7 cancer cells.

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Breast cancer is commonly treated with anti-estrogens or aromatase inhibitors, but resistant disease eventually develops and new therapies for such resistance are of great interest. We have previously isolated several tamoxifen-resistant variant sub-lines of the MCF-7 breast cancer cell line and

2,6-Bis((3,4-dihydroxyphenyl)-methylene)cyclohexanone (BDHPC)-induced apoptosis and p53-independent growth inhibition: synergism with genistein.

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Estrogen binds to two classes of proteins in the cells, the high-affinity estrogen receptor (ER) as well as a low affinity estrogen type II binding site (EBS-II). Methyl p-hydroxyphenyllactate (MeHPLA) is an endogenous ligand for EBS-II. Binding of MeHPLA to EBS-II has a growth regulatory effect in

Synthesis and cytotoxic potential of heterocyclic cyclohexanone analogues of curcumin.

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A series of 18 heterocyclic cyclohexanone analogues of curcumin have been synthesised and screened for their activity in both adherent and non-adherent cancer cell models. Cytotoxicity towards MBA-MB-231 breast cancer cells, as well as ability to inhibit NF-kappaB transactivation in non-adherent

Volatile organic metabolites identify patients with breast cancer, cyclomastopathy, and mammary gland fibroma.

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The association between cancer and volatile organic metabolites in exhaled breaths has attracted increasing attention from researchers. The present study reports on a systematic study of gas profiles of metabolites in human exhaled breath by pattern recognition methods. Exhaled breath was collected

Synthesis of new uracil derivatives and their sugar hydrazones with potent antimicrobial, antioxidant and anticancer activities.

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6-(4-Chloro-3-nitrophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile (4) was prepared and was reacted with ethyl chloroacetate, hydrazine hydrate, 4-chloroaniline, formaldehyde, acetic anhydride, formic acid, carbon disulfide, 4-cyanobenzaldehyde, triethyl orthoformate,

The study of a curcumin-resembling molecular probe for the pH-responsive fluorometric assay and application in cell imaging.

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A molecular probe of DibOH (2,6-bis(4-hydroxybenzylidene)cyclohexanone) designed as the ameliorant to the curcumin was prepared in which one enol unit was removed to avoid the intramolecular hydrogen bond and thus more rigidity and better coplanarity were achieved. Deprotonation of the phenolic

Combination therapy with a nuclear type-ii site agonist and 5-Fluorouracil - inhibition of mammary-tumor growth.

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Methyl p-hydroxyphenyllactate (MeHPLA) is an endogenous ligand for nuclear type II sites which apparently regulates cellular growth and proliferation through this binding interaction. Occupancy of type II sites by MeHPLA agonists such as dihydroxybenzylidene acetophenone (DHBA), 2,6-bis

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

Synthesis of new spirooxindole-pyrrolothiazole derivatives: Anti-cancer activity and molecular docking.

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The 1,3-dipolar cycloadditions of an azomethine ylide generated from isatin and thiazolidinecarboxylic acid to a series of 2,6-bis[(E)-arylmethylidene]cyclohexanones afforded new di-spiro heterocycles incorporating pyrrolidine and oxindole rings in quantitative yields and chemo-, regio-, and

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