Synthesis and Biological Evaluation of Substituted 3-anilino-quinolin-2(1H)-ones as PDK1 Inhibitors
| avondale-bepress.context-key | 6888295 | |
| avondale-bepress.submission-path | sci_math_papers/62 | |
| 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 | 2014-07-15 | |
| dc.date.submitted | 2015-03-23T21:53:04Z | |
| dc.description.abstract | <p>PDK1 is an important regulator of the PI3K/Akt pathway, which has been found frequently activated in a large number of human cancers. Herein we described the preparation of novel substituted 3-anilino-quinolin-2(1<em>H</em>)-ones as PDK1 inhibitors. The synthesis is based around a Buchwald–Hartwig cross-coupling of various 3-bromo-6-substituted-quinolin-2(1<em>H</em>)-ones with three different functionalised anilines. The modular nature of the designed synthesis allowed access to a series of novel inhibitors through derivatisation of a late-stage intermediate. All compounds were screened against isolated PDK1 enzyme, 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 3-anilino-quinolin-2(1H)-ones as PDK1 inhibitors. <em>Bioorganic and Medicinal Chemistry, 22</em>(14), 3781-3790. doi:10.1016/j.bmc.2014.04.037</p> | |
| dc.identifier.doi | https://doi.org/10.1016/j.bmc.2014.04.037 | |
| dc.identifier.issn | 0968-0896 | |
| dc.identifier.uri | https://research.avondale.edu.au/handle/1897/06888295 | |
| 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 3-anilino-quinolin-2(1H)-ones as PDK1 inhibitors. <em>Bioorganic and Medicinal Chemistry, 22</em>(14), 3781-3790. doi:10.1016/j.bmc.2014.04.037</p> <p>ISSN:0968-0896</p> | |
| dc.relation.ispartof | Bioorganic and Medicinal Chemistry | |
| dc.rights | <p>Due to copyright restrictions this article is unavailable for download.</p> <p>Copyright © 2014 Published by Elsevier Ltd. All rights reserved.</p> | |
| dc.subject | 3-Phosphoinositide-dependent kinase 1 (PDK1) | |
| dc.subject | 3-Anilino-quinolin-2(1H)-ones Inhibitor | |
| dc.subject | Buchwald–Hartwig cross-coupling | |
| dc.subject | Cross-coupling | |
| dc.title | Synthesis and Biological Evaluation of Substituted 3-anilino-quinolin-2(1H)-ones as PDK1 Inhibitors | |
| dc.type | Journal Article |