- Design, synthesis and preliminary biological evaluation of acridine compounds as potential agents for a combined targeted chemo-radionuclide therapy approach to melanoma
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Various iodo-acridone and acridine carboxamides have been prepared and evaluated as agents for targeted radionuclide and/or chemotherapy for melanoma, due to their structural similarity to benzamides which are known to possess specific affinity for melanin. Three of these carboxamides selected for their in vitro cytotoxic properties were radioiodinated with [125I]NaI at high specific activity. Biodistribution studies carried out in B16F0 murine melanoma tumour-bearing mice highlighted that acridone 8f and acridine 9d, presented high, long-lasting tumour concentrations together with an in vivo kinetic profile favourable to application in targeted radionuclide therapy.
- Desbois, Nicolas,Gardette, Maryline,Papon, Janine,Labarre, Pierre,Maisonial, Aurelie,Auzeloux, Philippe,Lartigue, Claire,Bouchon, Bernadette,Debiton, Eric,Blache, Yves,Chavignon, Olivier,Teulade, Jean-Claude,Maublant, Jean,Madelmont, Jean-Claude,Moins, Nicole,Chezal, Jean-Michel
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p. 7671 - 7690
(2008/12/23)
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- Pyridazinedione compounds useful in treating neurological disorders
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The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.
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- Nickel Boride Reduction of Aryl Nitro Compounds
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Nickel boride smoothly reduces aryl nitro compounds to the corresponding anilines in the presence of iodo and ortho carboalkoxy groups in contrast to the problematic reductions by other methods.
- Seltzman, Herbert H.,Berrang, Bertold D.
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p. 3083 - 3086
(2007/10/02)
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