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  • Title: Synthesis and biological evaluation of 2-anilino-4-substituted-7H-pyrrolopyrimidines as PDK1 inhibitors.
    Author: O'Brien NJ, Brzozowski M, Buskes MJ, Deady LW, Abbott BM.
    Journal: Bioorg Med Chem; 2014 Aug 01; 22(15):3879-86. PubMed ID: 25012568.
    Abstract:
    PDK1, a biological target that has attracted a large amount of attention recently, is responsible for the positive regulation of the PI3K/Akt pathway that is often activated in a large number of human cancers. A series of second-generation 2-anilino-4-substituted-7H-pyrrolopyrimidines were synthesised by installation of various functions at the 4-position of the 7H-pyrrolopyrimidine scaffold. All compounds were screened against the isolated PDK1 enzyme and dose response analysis was obtained on the best compounds of the series.
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