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.
Keywords: 2-Anilino-4-substituted-pyrrolopyrimidines; 3-Phosphoinositide-dependent kinase 1 (PDK1); Buchwald–Hartwig cross-coupling; Inhibitor; Suzuki cross-coupling.
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