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Discovery of pyrrolopyrimidine inhibitors of Akt.

Blake, James F; Kallan, Nicholas C; Xiao, Dengming; Xu, Rui; Bencsik, Josef R; Skelton, Nicholas J; Spencer, Keith L; Mitchell, Ian S; Woessner, Richard D; Gloor, Susan L; Risom, Tyler; Gross, Stefan D; Martinson, Matthew; Morales, Tony H; Vigers, Guy P A; Brandhuber, Barbara J.
Bioorg Med Chem Lett; 20(19): 5607-12, 2010 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-20810279
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.
Selo DaSilva