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phenanthrene/рак молочной железы
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Substituted phenanthrenes with basic amino side chains: a new series of anti-breast cancer agents.
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In the course of our search for new anti-breast cancer agents, substituted phenanthrenes with basic amino side chains were synthesized and some of them showed remarkable antiproliferative activity against ER +ve MCF-7 cell line with IC(50) in the range of 3.53-22.25 microM. One of the compounds 15
Synthesis of substituted phenanthrene-9-benzimidazole conjugates: Cytotoxicity evaluation and apoptosis inducing studies.
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A series of new phenanthrene-9-benzimidazole conjugates has been synthesized by condensing phenanthrene aldehydes with various substituted o-phenylenediamines. The title compounds were evaluated for their in vitro cytotoxic potential against various human cancer cell lines like breast (BT-549),
Differential action of chlorinated polycyclic aromatic hydrocarbons on aryl hydrocarbon receptor-mediated signaling in breast cancer cells.
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Chlorinated polycyclic aromatic hydrocarbons (ClPAHs), which are a series of halogenated aromatic hydrocarbons, have been found in the environment. The primary step in their metabolic activation seems to be associated with aryl hydrocarbon receptor (AhR)-mediated induction of the cytochrome P450
Development of a methodology to quantify tamoxifen and endoxifen in breast cancer patients by micellar liquid chromatography and validation according to the ICH guidelines.
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A simple micellar liquid chromatographic procedure is described to determine tamoxifen and endoxifen in plasma. For the analysis, tamoxifen and endoxifen solutions were diluted in water and UV-irradiated for 20 min to form the photocycled derivative with a phenanthrene core which shows intense
Tamoxifen monitoring studies in breast cancer patients by micellar liquid chromatography.
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A simple micellar liquid chromatographic procedure is described to determine tamoxifen in plasma. To perform the analysis, tamoxifen solutions were diluted in water and UV-irradiated for 20 min to form the photocycled derivative with a phenanthrene core which shows intense fluorescence. Samples were
Synthetic, crystallographic, computational, and biological studies of 1,4-difluorobenzo[c]phenanthrene and its metabolites.
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1,4-Difluorobenzo[c]phenanthrene (1,4-DFBcPh) and its putative metabolites, the dihydrodiol and diol epoxides, have been synthesized and structurally characterized, and the extent of DNA binding by the metabolites has been assessed. 1,4-DFBcPh and 1,4-difluoro-10-methoxybenzo[c]phenanthrene were
Synthesis and biological evaluation of phenanthrenes as cytotoxic agents with pharmacophore modeling and ChemGPS-NP prediction as topo II inhibitors.
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In a structure-activity relationship (SAR) study, 3-methoxy-1,4-phenanthrenequinones, calanquinone A (6a), denbinobin (6b), 5-OAc-calanquinone A (7a) and 5-OAc-denbinobin (7b), have significantly promising cytotoxicity against various human cancer cell lines (IC(50) 0.08-1.66 µg/mL). Moreover, we
Synthesis and in vitro Cytotoxicity Evaluation of Phenanthrene Linked 2,4-Thiazolidinediones as Potential Anticancer Agents
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Objective: To synthesize a series of phenanthrene-thiazolidinedione hybrids and explore their cytotoxic potential against human cancer cell lines of A-549 (lung cancer), HCT-116 and HT-29 (colon cancer), MDA MB-231 (triple negative breast
Antitumor agents 253. Design, synthesis, and antitumor evaluation of novel 9-substituted phenanthrene-based tylophorine derivatives as potential anticancer agents.
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C9-Substituted phenanthrene-based tylophorine derivatives (PBTs) (13-36) were synthesized and evaluated as in vitro anticancer agents against the human A549 lung cancer cell line. Twelve active compounds were further examined against DU-145 (prostate), ZR-751 (breast), KB (nasopharyngeal), and
Atropisomeric bi(9,10-dihydro)phenanthrene and phenanthrene/bibenzyl dimers with cytotoxic activity from the pseudobulbs of Pleione bulbocodioides.
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Bulbocodioidins E-H (1-4), four pairs of undescribed racemic bi(9,10-dihydro)phenanthrene and phenanthrene/bibenzyl atropisomers, along with four known compounds (5-8) were isolated from the ethanol extract of the pseudobulbs of Pleione bulbocodioides. Their structures were established by HRESIMS
Tobacco smoke carcinogens and breast cancer.
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Cigarette smoking is an established cause of a variety of cancer types, but its role in breast cancer etiology is not clear. In this report, the potential role of cigarette smoke carcinogens as causes of human breast cancer is evaluated. Of over 60 known carcinogens in tobacco smoke, several are
Potential anticancer activity of tanshinone IIA against human breast cancer.
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Tanshinone IIA is a derivative of phenanthrene-quinone isolated from Danshen, a widely used Chinese herbal medicine. It has antioxidant properties and cytotoxic activity against multiple human cancer cell lines, inducing apoptosis and differentiation of some human cancer cell lines. Our purpose was
Structural characterization and biological effects of photocyclized products of tamoxifen irradiation.
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Tamoxifen (TAM) is an antiestrogen useful in the treatment and control of breast cancer. Exposure of solutions of TAM to UV irradiation produces mixtures of fluorescent derivatives that are useful in the analytical detection and quantitative determination of TAM. The two major products of such
Topographic recognition of cyclic hydrocarbons and related compounds by receptors for androgens, estrogens, and glucocorticoids.
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The structural requirements for the interaction of about 80 cyclic hydrocarbons and related compounds with the androgen receptor of rat ventral prostate, the estrogen receptor of human breast tumor MCF-7 cells, and the glucocorticoid receptor of rat liver were examined by comparing their abilities
Characterization of a major aromatic DNA adduct detected in human breast tissues.
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A bulky DNA adduct (Spot 1) was previously detected in normal adjacent breast tissues of 41% (36/87) of women with breast cancer and in none (0/29) of the noncancer controls by (32)P-postlabeling. To characterize this adduct, it was chromatographically compared with DNA adduct profiles generated in
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