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ID: ALA1255571

Journal: Bioorg Med Chem Lett

Title: Discovery of pyrrolopyrimidine inhibitors of Akt.

Authors: Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ.

Abstract: The discovery and optimization of a series of pyrrolopyrimidine based protein kinase B (Pkb/Akt) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent inhibition of all three Akt isoforms and knockdown of phospho-PRAS40 levels in LNCaP cells and tumor xenografts.

CiteXplore: 20810279

DOI: 10.1016/j.bmcl.2010.08.053