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Страница 1 от 20 резултата
Mitochondrial targeting for photochemotherapy. Can selective tumor cell killing be predicted based on n-octanol/water distribution coefficients?
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The concept of mitochondrial targeting for chemo- and photochemotherapy of neoplastic diseases has its origin in the observation that enhanced mitochondrial transmembrane potential is a common tumor cell phenotype. As a result of this enhanced transmembrane potential, a number of cationic dyes
Analogues of hexamethylmelamine. The anti-neoplastic activity of derivatives with enhanced water solubility.
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The preparation of some water soluble analogues of the tumour growth inhibitory hexamethylmelamine is described. The ultra-violet absorption characteristics, solubility and n-octanol/water partition coefficients of these new derivatives and some related compounds have been determined. Rates of
Effects of high-dose medroxyprogesterone acetate and various other steroid hormones on plasma membrane lipid mobility in CAMA-1 mammary cancer cells.
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The influence of medroxyprogesterone acetate (MPA) and various other steroid hormones on the lateral diffusion of the fluorescent lipid probe 1-acyl-2-(N-4-nitrobenzo-2-oxa-1.3-diazolyl)-aminocarpropylphos phatidylcholine (NBD-PC) in the plasma membrane of intact mammary cancer cells (CAMA-1 cell
Developing and Evaluating In Vitro Effect of Poly(Ethylene Glycol) Conjugated Curcumin on Human Cancer Cell Lines.
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Curcumin has been shown to possess strong cytotoxic effect against various cancer cell lines. However, curcumin has not applied as a drug for treatment of cancer yet due to low solubility in water and low bioavailability. The aims of this study were to prepare a new polyethylene glycol (PEG)
The activity of class I, II, III, and IV alcohol dehydrogenase isoenzymes and aldehyde dehydrogenase in colorectal cancer.
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Chronic ethanol consumption is associated with an increased risk for cancer of the colorectum. The highly toxic and carcinogenic compound is acetaldehyde, the product of ethanol metabolism. Ethanol is metabolized to acetaldehyde by alcohol dehydrogenase (ADH) in colorectal mucosa and bacteria. The
Preparation of (99m)Tc-labelled methotraxate by a direct labeling technique as a potential diagnostic agent for breast cancer and preliminary clinical results.
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Methotrexate (MTX) is being used in clinical oncology for the treatment of a wide variety of cancers. The aim of the present study was to label directly MTX with (99m)Tc by using Sn/pyrophosphate as reducing agent and to use this labeled compound as a potential anticancer radiopharmaceutical for
Cationic, linear Au(I) N-heterocyclic carbene complexes: synthesis, structure and anti-mitochondrial activity.
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Six linear, two-coordinate cationic Au(I) N-heterocyclic carbene complexes of the form [(R2Im)2Au]+ (R = Me 1, Me, Et 2, i-Pr 3, n-Bu 4, t-Bu 5 and Cy 6) have been prepared by the reaction of two equivalents of the appropriate dialkylimidazol-2-ylidene (R2Im) with (Me2S)AuCl in dmf. Single crystal
Novel skin penetrating berberine oleate complex capitalizing on hydrophobic ion pairing approach.
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Berberine hydrochloride (Brb) is a well-known herbal drug that holds a great promise in the recent years thanks to its various pharmacological actions. Currently, Brb is extensively researched as a natural surrogate with evidenced potentiality against numerous types of skin diseases including skin
In vitro cell studies of technetium-99m labeled RGD-HYNIC peptide, a comparison of tricine and EDDA as co-ligands.
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The level of alpha(V)beta(3) integrins on endothelial cells is elevated in angiogenesis. The high binding specificity to alpha(V)beta(3) integrins of peptides containing Arg-Gly-Asp (RGD) residues suggests that the radiolabeled RGD peptides may be useful as tumor specific imaging agents. In this
Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.
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In a continued effort to find a suitable PET tracer for visualization of angiogenic processes, we explored the 3,4-diarylmaleimide family, known to have high affinity and selectivity towards the VEGFR-TKs. One previously reported agent and three new halogen-containing 3,4-diarylmaleimide derivatives
Influence of pyridine versus piperidine ligands on the chemical, DNA binding and cytotoxic properties of light activated trans,trans,trans-[Pt(N3)2(OH)2(NH3)(L)].
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The photocytotoxicity and photobiochemical properties of the new complex trans,trans,trans-[Pt(N(3))(2)(OH)(2)(NH(3))(piperidine)] (5) are compared with its analogue containing the less basic and less lipophilic ligand pyridine (4). The log P (n-octanol/water) values were of -1.16 and -1.84 for the
A quantitative structure-activity approach for lipophilicity estimation of antitumor complexes of different metals using microemulsion electrokinetic chromatography.
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Microemulsion electrokinetic chromatography (MEEKC) offers a valuable tool for the rapid and highly productive determination of lipophilicity for metal-based anticancer agents. In this investigation, the MEEKC technique was applied for estimation of n-octanol-water partition coefficient (logP(oct))
Tuning the structure of aminoferrocene-based anticancer prodrugs to prevent their aggregation in aqueous solution.
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Aminoferrocene-based prodrugs are activated in cancer cells by reactive oxygen species (ROS). They were shown to exhibit high cytotoxicity towards a variety of cancer cell lines and primary cancer cells, but remain not toxic towards non-malignant cells. However, these prodrugs have rather high
In vitro and in vivo antitumour activity and cellular pharmacological properties of new platinum-iminoether complexes with different configuration at the iminoether ligands.
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In order to widen our knowledge on antitumour trans-[PtCl2(iminoether)2] complexes, we have synthesised two new derivatives, trans-[PtCl2¿E-HN = C(OEt)Me¿2] (1) and trans-[PtCl2¿Z-HN = C(OEt)Me¿2] (2), which differ in the configuration of the iminoether ligands. Isomer 1 showed an in vitro
Ambazone as a membrane active antitumor drug.
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Ambazone (1,4-benzoquinone guanylhydrazone thiosemicarbazone) was found to be active against various transplantable tumors in mice as well as rats. When administered orally for 4-9 days, the effective therapeutic dose ranged between 60 and 125 mg/kg. The antineoplastic effect of ambazone appeared to
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