Synthesis and Biological Evaluation of Substituted 2-anilino-7H-pyrrolopyrimidines as PDK1 Inhibitors
| avondale-bepress.context-key | 6907342 | |
| avondale-bepress.submission-path | sci_math_papers/64 | |
| avondale.faculty | Science | |
| avondale.reporting.isPeerReviewed | Peer Reviewed | |
| avondale.reporting.version | Published Version | |
| dc.contributor.author | Abbott, Belinda M. | |
| dc.contributor.author | Deady, Leslie W. | |
| dc.contributor.author | Wilson, David J. | |
| dc.contributor.author | Brzozowski, Martin | |
| dc.contributor.author | O'Brien, Nathan J. | |
| dc.date.accessioned | 2023-11-01T00:39:24Z | |
| dc.date.available | 2023-11-01T00:39:24Z | |
| dc.date.issued | 2014-05-21 | |
| dc.date.submitted | 2015-03-26T21:02:26Z | |
| dc.description.abstract | <p>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 BuchwaldeHartwig 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.</p> | |
| dc.identifier.citation | <p>O'Brien, N. J., Brzozowski, M., Wilson, D. J., Deady, L. W., & Abbott, B. M. (2014). Synthesis and biological evaluation of substituted 2-anilino-7H-pyrrolopyrimidines as PDK1 inhibitors. <em>Tetrahedron, 70</em>(33), 4947-4956. doi:10.1016/j.tet.2014.05.033</p> | |
| dc.identifier.issn | 0040-4020 | |
| dc.identifier.uri | https://research.avondale.edu.au/handle/1897/06907342 | |
| dc.language.iso | en_us | |
| dc.provenance | <p>This article was originally published as:</p> <p>O'Brien, N. J., Brzozowski, M., Wilson, D. J., Deady, L. W., & Abbott, B. M. (2014). Synthesis and biological evaluation of substituted 2-anilino-7H-pyrrolopyrimidines as PDK1 inhibitors. <em>Tetrahedron, 70</em>(33), 4947-4956. doi:10.1016/j.tet.2014.05.033</p> <p>ISSN:0040-4020</p> | |
| dc.relation.ispartof | Tetrahedron | |
| dc.rights | <p>Due to copyright restrictions this article is unavailable for download.</p> <p>Crown copyright © 2014 Published by Elsevier Ltd. All rights reserved.</p> <p>This article may be accessed from the publisher <a href="http://dx.doi.org/10.1016/j.tet.2014.05.033">here.</a></p> | |
| dc.subject | 3-Phosphoinositide-dependent kinase 1 (PDK1) | |
| dc.subject | 2-Anilino-7H-pyrrolopyrimidines | |
| dc.subject | Inhibitor | |
| dc.subject | Suzuki cross-coupling | |
| dc.subject | Buchwalde-Hartwig cross-coupling | |
| dc.title | Synthesis and Biological Evaluation of Substituted 2-anilino-7H-pyrrolopyrimidines as PDK1 Inhibitors | |
| dc.type | Journal Article |