Cycloalkyl-substituted aryl chloroethylureas inhibiting cell cycle progression in G 0/G 1 phase and thioredoxin-1 nuclear translocation

…, J Lacroix, A Patenaude, É Petitclerc, C René

Index: Fortin, Jessica S.; Cote, Marie-France; Lacroix, Jacques; Patenaude, Alexandre; Petitclerc, Eric; C.-Gaudreault, Rene Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 12 p. 3526 - 3531

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Citation Number: 10

Abstract

1-(2-Chloroethyl)-3-(4-cyclohexylphenyl) urea (cHCEU) has been shown to abrogate the presence of thioredoxin-1 into the nucleus through its selective covalent alkylation. In the present letter we have evaluated the structure–activity relationships of the substituents at positions 3 and 4 of the phenyl ring of cHCEU derivatives on cell cycle progression and thioredoxin-1 nuclear translocation. Active CEU derivatives exhibited GI50 ranging from ...