The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Discovery of 4-Amino-N-[(1 S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7 H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases
Open accessAbstract
Wide-ranging exploration of analogues of an ATP-competitive pyrrolopyrimidine inhibitor of Akt led to the discovery of clinical candidate AZD5363, which showed increased potency, reduced hERG affinity, and higher selectivity against the closely related AGC kinase ROCK. This compound demonstrated good preclinical drug metabolism and pharmacokinetics (DMPK) properties and, after oral dosing, showed pharmacodynamic knockdown of phosphorylation of Akt and downstream biomarkers in vivo, and inhibition of tumor growth in a breast cancer xenograft model.
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Cites
Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex
Sarbassov, D. D., Guertin, D. A., Ali, S. M., & Sabatini, D. M. (2005) · Science · doi:10.1126/science.1106148 · Cited by 6,216
AKT/PKB signaling: navigating downstream
Manning, B. D., & Cantley, L. C. (2007) · Cell · doi:10.1016/j.cell.2007.06.009 · Cited by 6,115
The nuts and bolts of AGC protein kinases
Pearce, L. R., Komander, D., & Alessi, D. R. (2010) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2822 · Cited by 1,294
Cited by
Twenty years on: the impact of fragments on drug discovery
Erlanson, D. A., Fesik, S. W., Hubbard, R. E., Jahnke, W., & Jhoti, H. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.109 · Cited by 1,000
Molecular targets for cancer therapy in the PI3K/AKT/mTOR pathway
Polivka, J., & Janku, F. (2014) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2013.12.004 · Cited by 765
Tumor biomarkers for diagnosis, prognosis and targeted therapy
Zhou, Y., Tao, L., Qiu, J., Xu, J., Yang, X., Zhang, Y., Tian, X., Guan, X., Cen, X., & Zhao, Y. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-01823-2 · Cited by 720
Targeting the PI3K/AKT/mTOR pathway in triple-negative breast cancer: a review
Costa, R. L. B., Han, H. S., & Gradishar, W. J. (2018) · Breast Cancer Research and Treatment · doi:10.1007/s10549-018-4697-y · Cited by 439
Molecular photoswitches in aqueous environments
Volarić, J., Szymanski, W., Simeth, N. A., & Feringa, B. L. (2021) · Chemical Society Reviews · doi:10.1039/d0cs00547a · Cited by 438
Metadata
- Authors
- Addie, M., Ballard, P., Buttar, D., Crafter, C., Currie, G., Davies, B. R., Debreczeni, J., Dry, H., Dudley, P., Greenwood, R., Johnson, P. D., Kettle, J. G., Lane, C., Lamont, G., Leach, A., Luke, R. W. A., Morris, J., Ogilvie, D., Page, K., Pass, M., Pearson, S., & Ruston, L.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2013-02-26
- Volume
- 56
- Issue
- 5
- Pages
- 2059-2073
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2037207588
- Cited by
- 230
- References
- 3
- FWCI
- 4.44
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Discovery of 4-Amino-N-[(1 S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7 H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases. https://app.cochat.ai/papers/10.1021/jm301762v
- The paper
- Addie, M., Ballard, P., Buttar, D., Crafter, C., Currie, G., Davies, B. R., Debreczeni, J., Dry, H., Dudley, P., Greenwood, R., Johnson, P. D., Kettle, J. G., Lane, C., Lamont, G., Leach, A., Luke, R. W. A., Morris, J., Ogilvie, D., Page, K., . . . Ruston, L. (2013). Discovery of 4-Amino-N-[(1 S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7 H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm301762v
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
