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Development of chemical probes: Toward the mode of action of a methylene-linked di(aryl acetate) E1

Smith, MEB; Gunn, RM; Rosivatz, E; Mak, LH; Woscholski, R; Hailes, HC; (2010) Development of chemical probes: Toward the mode of action of a methylene-linked di(aryl acetate) E1. BIOORGAN MED CHEM , 18 (14) 4917 - 4927. 10.1016/j.bmc.2010.06.017.

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Abstract

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.

Type:Article
Title:Development of chemical probes: Toward the mode of action of a methylene-linked di(aryl acetate) E1
DOI:10.1016/j.bmc.2010.06.017
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 > Faculty of Maths and Physical Sciences > Chemistry

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