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.
Copyright © 2011 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Cell Proliferation / drug effects
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Chemistry Techniques, Synthetic*
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Choline Kinase / antagonists & inhibitors
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Electron Transport
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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HT29 Cells
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Humans
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Inhibitory Concentration 50
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Oxazoles / chemical synthesis
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Oxazoles / chemistry*
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Oxazoles / pharmacology*
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Pyridines / chemistry*
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Salts / chemistry*
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Oxazoles
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Pyridines
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Salts
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Choline Kinase
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pyridine