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  • Title: Bispyridinium cyclophanes: novel templates for human choline kinase inhibitors.
    Author: Conejo-García A, Campos JM, Sánchez-Martín RM, Gallo MA, Espinosa A.
    Journal: J Med Chem; 2003 Aug 14; 46(17):3754-7. PubMed ID: 12904080.
    Abstract:
    The synthesis and biological activities of four novel bispyridinium cyclophanes as choline kinase (ChoK) inhibitors are presented. Their synthetic methodology has been optimized according to dilution, temperature, and reaction time and provides pure bispyridinium cyclophanes in high yields very easily. One of these cyclophanes (6, 4,8-diaza-3(1,4),9(4,1)-dipyridina-1(1,4),6(1,3)-dibenzenacyclodecaphan-3(1),9(1)-bis(ilium) dibromide) has an IC(50(ChoK)) of 0.3 microM and is the most potent human ChoK inhibitor described to date.
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