Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 36, Issue 3, Pages 215-225Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/S0223-5234(01)01219-3
Keywords
antiproliferative agents; electrostatic effects; choline kinase; quantitative structure-activity relationship
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Eleven derivatives of 1,1'-[1,2-ethylenebis(benzene 1,4-diylmetXlylene)]bis(4-pyridinium) dibromides bearing various groups at C-4 of the pyridinium moiety were synthesized and examined for their inhibition of choline kinase (ChoK) and antiproliferative activities. The C-4 substituents include electron-releasing, neutral or electron-withdrawing groups. A one-parameter regression equation has been derived which satisfactorily describes the ex vivo inhibitory potency of ChoK of the title compounds. The electronic effect plays a critical function in the ex vivo inhibition of ChoK although the role of electrostatic interactions could be altered due to a solvation process of both ChoK and ligands. (C) 2001 Editions scientifiques et medicales Elsevier SAS.
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