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

…, E Rosivatz, LH Mak, R Woscholski, HC Hailes

文献索引:Smith, Mark E.B.; Gunn, Richard M.; Rosivatz, Evelyn; Mak, Lok H.; Woscholski, Ruediger; Hailes, Helen C. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 14 p. 4917 - 4927

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摘要

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 ...