1498710-52-3Relevant academic research and scientific papers
Synthesis and biological evaluation of substituted 2-anilino-7H- pyrrolopyrimidines as PDK1 inhibitors
O'Brien, Nathan J.,Brzozowski, Martin,Wilson, David J.D.,Deady, Leslie W.,Abbott, Belinda M.
, p. 4947 - 4956 (2014/07/07)
An efficient and scalable route for a series of novel substituted 2-anilino-7H-pyrrolopyrimidine compounds as potential inhibitors of PDK1, an important regulator of the PI3K/Akt pathway that is dysregulated in many cancers, was developed and is described. The synthetic strategy was designed around Suzuki and Buchwald-Hartwig cross-couplings of a boronate fragment and various customised anilines sequentially with 2,4-dichloro-7-tosyl-7H- pyrrolopyrimidine. All fragments were constructed separately and cross-coupled to provide access to a range of novel compounds. Biological evaluation of these was undertaken, with modest inhibition observed.
