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Inhibition of the interactions between metastatic human breast cancer cells and platelets by β-nitrostyrene derivatives.

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OBJECTIVE The interactions between cancer cells and platelets have been recognized to play an important role in cancer progress as well as metastasis, and interference with cancer-platelet interactions is an attractive strategy for cancer therapy. In the present study, two β-nitrostyrene

Inhibitory effects of herbal extracts on breast cancer resistance protein (BCRP) and structure-inhibitory potency relationship of isoflavonoids.

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The inhibition of intestinal breast cancer resistance protein (BCRP), which restricts the absorption of xenobiotics, may increase the systemic availability of its substrates. The aim of this study was to evaluate the inhibitory effects of herbal extracts and their constituents on BCRP-mediated

Natural product ginsenoside 25-OCH3-PPD inhibits breast cancer growth and metastasis through down-regulating MDM2.

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Although ginseng and related herbs have a long history of utility for various health benefits, their application in cancer therapy and underlying mechanisms of action are not fully understood. Our recent work has shown that 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol (25-OCH(3)-PPD), a newly

25-methoxyl-dammarane-3β, 12β, 20-triol and artemisinin synergistically inhibit MDA-MB-231 cell proliferation through downregulation of testes-specific protease 50 (TSP50) expression.

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While the incidence of cancer continues to increase, the current therapeutic options remain imperfect. Therefore, there is an urgent need to discover new targeted anti-cancer therapies. Testes-specific protease 50 (TSP50) is abnormally expressed in most cancer tissues and downregulation of TSP50

New structure-activity relationships of chalcone inhibitors of breast cancer resistance protein: polyspecificity toward inhibition and critical substitutions against cytotoxicity.

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Adenosine triphosphate-binding cassette subfamily G member 2 (ABCG2) plays a major role in cancer cell multidrug resistance, which contributes to low efficacy of chemotherapy. Chalcones were recently found to be potent and specific inhibitors, but unfortunately display a significant cytotoxicity. A

Isolation, structural determination, and evaluation of the biological activity of 20(S)-25-methoxyl-dammarane-3beta, 12beta, 20-triol [20(S)-25-OCH3-PPD], a novel natural product from Panax notoginseng.

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Ginseng has been used extensively for medicinal purposes, with suggested utility for indications as diverse as diabetes, cardiovascular disease and cancer. Herein we report the discovery and characterization of 20(S)-25-OCH3-PPD, a ginsenoside that inhibits growth and survival of cancer cells. The

A synthetic chalcone as a potent inducer of glutathione biosynthesis.

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Chalcones continue to attract considerable interest due to their anti-inflammatory and antiangiogenic properties. We recently reported the ability of 2',5'-dihydroxychalcone (2',5'-DHC) to induce both breast cancer resistance protein-mediated export of glutathione (GSH) and c-Jun N-terminal

Homoisoflavanones with estrogenic activity from the rhizomes of Polygonatum sibiricum.

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A new homoisoflavanone, (3R)-5-hydroxy-7-methoxyl-3-(2'-hydroxy-4'- methoxybenzyl)-chroman-4-one (1), together with six known analogs, were isolated from the rhizomes of Polygonatum sibiricum. Their structures were elucidated on the basis of extensive spectroscopic analysis. All compounds were

Facile Synthesis of Resveratrol Nanogels with Enhanced Fluorescent Emission.

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Herein, a kind of fluorescent resveratrol nanogels via one-pot thiol-ene Michael addition polymerization of resveratrol triacrylate, 1,6-hexanedithiol, and methoxyl poly(ethylene glycol) acrylate is prepared. The resultant nanogels can be well-dispersed in water with a hydrodynamic radius of around

Resveratrol structure and ceramide-associated growth inhibition in prostate cancer cells.

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Resveratrol (3,4',5-trans-trihydroxystilbene) is a dietary polyphenol with chemopreventive properties present in grapes, red wine, peanuts and other edible products. The antiproliferative and proapoptotic effect of resveratrol in breast cancer cells can be traced to the accumulation of ceramide. In

Exploring the PROTAC degron candidates: OBHSA with different side chains as novel selective estrogen receptor degraders (SERDs).

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As the mutant estrogen receptor (ER) continues to be characterized, breast cancer is becoming increasingly difficult to cure when treated with hormone therapy. In this regard, a strategy to selectively and effectively degrade the ER might be an effective alternative to endocrine therapy for breast

Synthesis of 1,1,2-triphenylethylenes and their antiproliferative effect on human cancer cell lines.

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Tamoxifen analogs (1-3) and 1,1,2-triphenylethylenes (4-7) have been synthesized by the McMurry coupling reaction. Their antiproliferative effects on MCF-7 human breast-cancer cells, HO-8910 human ovarian-carcinoma cells, and (HL)-60 human promyelocytic-leukemia cells were studied by use of the

Biochemical and computational insights into the anti-aromatase activity of natural catechol estrogens.

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High levels of endogenous estrogens are associated with increased risks of breast cancer. Estrogen levels are mainly increased by the activity of the aromatase enzyme and reduced by oxidative/conjugative metabolic pathways. In this paper, we demonstrate for the first time that catechol estrogen

Exploitation of new chalcones and 4H-chromenes as agents for cancer treatment.

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Chalcone and chromene derivatives were synthesized in good yield through simple and effective reactions using innocuous solvents such as water and ethanol and high yielding aldol condensations. Generally, the reactions were performed at room temperature, leading to the isolation of highly pure

Discovery, synthesis and biological evaluation of cycloprotoberberine derivatives as potential antitumor agents.

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A series of new 1,13-cycloprotoberberine derivatives defined through variations at the 9-position were designed, synthesized and evaluated for their cytotoxicities in human HepG2 (hepatoma), HT1080 (fibrosarcoma) and HCT116 (colon cancer) cells. The preliminary structure-activity relationship (SAR)

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