di-2-pyridylketone-4-4-dimethyl-3-thiosemicarbazone and Neuroectodermal-Tumors--Primitive--Peripheral

di-2-pyridylketone-4-4-dimethyl-3-thiosemicarbazone has been researched along with Neuroectodermal-Tumors--Primitive--Peripheral* in 1 studies

Other Studies

1 other study(ies) available for di-2-pyridylketone-4-4-dimethyl-3-thiosemicarbazone and Neuroectodermal-Tumors--Primitive--Peripheral

ArticleYear
Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
    Journal of medicinal chemistry, 2010, Feb-11, Volume: 53, Issue:3

    Desferrioxamine B (DFOB) conjugates with adamantane-1-carboxylic acid, 3-hydroxyadamantane-1-carboxylic acid, 3,5-dimethyladamantane-1-carboxylic acid, adamantane-1-acetic acid, 4-methylphenoxyacetic acid, 3-hydroxy-2-methyl-4-oxo-1-pyridineacetic acid (N-acetic acid derivative of deferiprone), or 4-[3,5-bis(2-hydroxyphenyl)-1,2,4-triazol-1-yl]benzoic acid (deferasirox) were prepared and the integrity of Fe(III) binding of the compounds was established from electrospray ionization mass spectrometry and RP-HPLC measurements. The extent of intracellular (59)Fe mobilized by the DFOB-3,5-dimethyladamantane-1-carboxylic acid adduct was 3-fold greater than DFOB alone, and the IC(50) value of this adduct was 6- or 15-fold greater than DFOB in two different cell types. The relationship between logP and (59)Fe mobilization for the DFOB conjugates showed that maximal mobilization of intracellular (59)Fe occurred at a logP value approximately 2.3. This parameter, rather than the affinity for Fe(III), appears to influence the extent of intracellular (59)Fe mobilization. The low toxicity-high Fe mobilization efficacy of selected adamantane-based DFOB conjugates underscores the potential of these compounds to treat iron overload disease in patients with transfusional-dependent disorders such as beta-thalassemia.

    Topics: Adamantane; Administration, Oral; Animals; Binding Sites; Carboxylic Acids; Cell Proliferation; Cells, Cultured; Chelating Agents; Chromatography, High Pressure Liquid; Crystallography, X-Ray; Deferoxamine; Dogs; Ferric Compounds; Humans; Inhibitory Concentration 50; Iron; Iron Chelating Agents; Iron Overload; Kidney; Models, Molecular; Molecular Structure; Neuroectodermal Tumors, Primitive, Peripheral; Spectrometry, Mass, Electrospray Ionization; Structure-Activity Relationship; Transferrin

2010