Journal article
Synthesis and biological evaluation of 2-anilino-4-substituted-7H- pyrrolopyrimidines as PDK1 inhibitors
NJ O'Brien, M Brzozowski, MJ Buskes, LW Deady, BM Abbott
Bioorganic and Medicinal Chemistry | PERGAMON-ELSEVIER SCIENCE LTD | Published : 2014
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. Crown Copyright © 2014 Published by Elsevier Ltd. All rights reserved.
Grants
Funding Acknowledgements
The authors would like to thank Dr. Suzanne Cutts (La Trobe Institute for Molecular Science, La Trobe University) for her assistance with the biological assays and Dr. Jason Dang (Monash Institute of Pharmaceutical Sciences, Monash University) for HRMS analysis. N.J. O'Brien would like to thank the Australian government for financial support through the provision of an Australian Postgraduate Awards (APA) scholarship.