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Bromine- and iodine-substituted 16alpha,17alpha-dioxolane progestins for breast tumor imaging and radiotherapy: synthesis and receptor binding affinity.
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Progesterone receptors (PRs) are present in many breast tumors, and their levels are increased by certain endocrine therapies. We describe the synthesis and PR binding affinities of a series of bromine- and iodine-substituted 16alpha,17alpha-dioxolane progestins, some of which, when appropriately
The bromine enhancement ratio in mammalian cells in vitro and experimental mouse tumours.
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Human kidney cells in culture and cells of mouse sarcoma-180 were allowed to incorporate bromine into their DNA. Cultured cells with and without incorporated BUdR were irradiated with electromagnetic radiations ranging in energy from 12 keV X-rays to 60Co gamma-rays to find out whether or not there
Photophysical, photochemical, and tumor-selectivity properties of bromine derivatives of rhodamine-123.
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The conceptual basis for the development of mitochondrial targeting as a novel therapeutic strategy for both chemotherapy and photochemotherapy of neoplastic diseases rests on the observation that enhanced mitochondrial membrane potential is a common tumor cell phenotype. The potential of this
Comparative PET imaging of experimental tumors with bromine-76-labeled antibodies, fluorine-18-fluorodeoxyglucose and carbon-11-methionine.
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The potential of a 76Br-labeled anti-carcinoembryonic antigen monoclonal antibody (MAb), 38S1, as tumor-imaging agent for PET was investigated in a comparative experimental study with [18F]fluorodeoxyglucose ([18F]FDG) and L-[methyl-11C]methionine ([11C]Met).
METHODS
The three radiotracers were
[Study of toxicity and anti-tumor activity of mixtures of bromine, iodine- and fluorine-containing di-2-halogenethylamines].
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Trace element changes in serum and skeletal muscle compared to tumour tissue in sarcoma-bearing rats.
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Cancer cachexia is characterized by wasting of the lean tissue and profound changes in the body composition of the tumour host. These changes are partly explained by an inefficient energy production but other factors may also be important, such as deficiency of essential nutritional components. In
Oral iodine toxicity in chicks can be reversed by supplemental bromine.
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Four chick bioassays were conducted to quantify iodine (I) toxicity and its amelioration in young chicks. A supplemental I level from KI of 600 mg/kg depressed growth in chicks fed methionine-deficient diets but not in those fed methionine-adequate diets. An I dose level >or= 900 mg/kg was required
New Methods for Labeling RGD Peptides with Bromine-76.
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Direct bromination of the tyrosine residues of peptides and antibodies with bromine-76, to create probes for PET imaging, has been reported. For peptides that do not contain tyrosine residues, however, a prosthetic group is required to achieve labeling via conjugation to other functional groups such
Health risk assessment and soil and plant heavy metal and bromine contents in field plots after ten years of organic and mineral fertilization.
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Heavy metals and bromine (Br) derived from organic and industrialized fertilizers can be absorbed, transported and accumulated into parts of plants ingested by humans. This study aimed to evaluate in an experiment conducted under no-tillage for 10 years, totaling 14 applications of pig slurry manure
Pharmacokinetics and experimental PET imaging of a bromine-76-labeled monoclonal anti-CEA antibody.
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Bromine-76 is potentially useful as a radiolabel for monoclonal antibodies (MAbs) in PET imaging. The purpose of the present study was to evaluate the 76Br-labeled anticarcinoembryonic antigen (-CEA) MAb 38S1 as a tumor imaging agent in an experimental tumor model and to study the pharmacokinetics
[Tumor imaging with conventional X-ray using a new artificial blood substitute (perfluoroctylbromide emulsion, FOB)].
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A new artificial blood substitute, FOB, which has been shown to be a good solvent for oxygen, contains a Bromine atom within its molecule. FOB is taken up in tumor macrophages and the Bromine shows opacity on X-ray film by absorbance of X-rays. In this study, tumor imaging possibilities were studied
[125I/127I/131I]Iodorhodamine: synthesis, cellular localization, and biodistribution in athymic mice bearing human tumor xenografts and comparison with [99mTc]hexakis(2-methoxyisobutylisonitrile).
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The synthesis of halogenated rhodamine (Rh) derivatives was carried out by controlling the stoichiometry of the halogenating agents, bromine and iodine monochloride. In the no-carrier-added synthesis of radioiodinated rhodamine 123, direct labeling of rhodamine 123 (Rh 123) with Na125I/Na131I
In vitro assessment of intestinal permeability and hepatic metabolism of 4'-bromoflavone, a promising cancer chemopreventive agent.
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1. The intestinal permeability and hepatic metabolism of the investigational cancer chemoprevention agent 4'-bromoflavone were investigated in vitro using human intestinal Caco-2 cell monolayers, human liver microsomes and human hepatocytes. Liquid chromatography-mass spectrometry and tandem mass
Regenerative hyperplasia is not required for liver tumor induction in female B6C3F1 mice exposed to trihalomethanes.
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Chloroform (TCM), a water disinfection by-product, induced liver tumors in female mice when administered by gavage in corn oil but not when given in drinking water at comparable daily doses. Because short-term studies showed that the gavage doses also induced liver toxicity, it has been suggested
Inhibition of microtubule assembly in tumor cells by 3-bromoacetylamino benzoylurea, a new cancericidal compound.
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We have synthesized a new compound, 3-bromoacetylamino benzoylurea (3-BAABU), which showed strong cancericidal activity by inducing irreversible mitotic arrest and subsequently apoptosis in human T cell leukemic cells (CEM), human biphenotypic leukemic cells (SP), a human prostate cancer cell line
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