Development of chemical probes: Toward the mode of action of a methylene-linked di(aryl acetate) E1.
BIOORGAN MED CHEM
4917 - 4927.
Analogues of the novel inhibitor of the PI3-K/PKB pathway, 2-[5-(2-chloroethyl)-2-acetoxy-benzyl]-4-(2-chloroethyl)-phenyl acetate (E1), have been prepared and preliminary SAR performed. This established that at least one of the chloroethyl para-substituents could be removed or modified and the ability to inhibit PKB/Akt activation retained. Synthetic methodologies were then developed to methylene-linked aryl acetates for use as molecular probes to identify the target of compound E1. (C) 2010 Elsevier Ltd. All rights reserved.
|Title:||Development of chemical probes: Toward the mode of action of a methylene-linked di(aryl acetate) E1|
|Keywords:||PI3-K/PKB inhibitors, PKB/Akt, Biotin conjugates, Methylene-linked aryls, Molecular probes, CARBON BOND FORMATION, DERIVATIVES, PHENOLS, HALIDES, COMPOUND-48/80, FORMALDEHYDE, ACTIVATION, INHIBITOR, CATALYSIS, REAGENTS|
|UCL classification:||UCL > School of BEAMS
UCL > School of BEAMS > Faculty of Maths and Physical Sciences
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