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Eur J Med Chem ; 46(11): 5662-7, 2011 Nov.
Article in English | MEDLINE | ID: mdl-21996467

ABSTRACT

A series of bispyridinium compounds were synthesized by a short sequence of reactions from symmetric diamides. All compounds were tested for their antiproliferative activity against HT-29, a cell line derived from a human colon adenocarcinoma, and their inhibitory activity against choline kinase (ChoK), a novel anticancer molecular target already in clinical trials. Most of the compounds analyzed showed good antiproliferative activities, in the micromolar range, with the identification of promising lead molecules as a new family of potential inhibitors of ChoK.


Subject(s)
Chemistry Techniques, Synthetic , Oxazoles/chemistry , Oxazoles/pharmacology , Pyridines/chemistry , Salts/chemistry , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Proliferation/drug effects , Choline Kinase/antagonists & inhibitors , Electron Transport , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , HT29 Cells , Humans , Inhibitory Concentration 50 , Oxazoles/chemical synthesis
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