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Diaryl- and triaryl-pyrrole derivatives: inhibitors of the MDM2–p53 and MDMX–p53 protein–protein interactions
Screening identified 2-(3-((4,6-dioxo-2-thioxotetrahydropyrimidin-5(2H)-ylidene)methyl)-2,5-dimethyl-1H-pyrrol-1-yl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile as an MDM2–p53 inhibitor (IC(50) = 12.3 μM). MDM2–p53 and MDMX–p53 activity was seen for 5-((1-(4-chlorophenyl)-2,5-diphenyl-1H-pyrr...
Autores principales: | Blackburn, Tim J., Ahmed, Shafiq, Coxon, Christopher R., Liu, Junfeng, Lu, Xiaohong, Golding, Bernard T., Griffin, Roger J., Hutton, Claire, Newell, David R., Ojo, Stephen, Watson, Anna F., Zaytzev, Andrey, Zhao, Yan, Lunec, John, Hardcastle, Ian R. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Royal Society of Chemistry
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3777193/ https://www.ncbi.nlm.nih.gov/pubmed/24078862 http://dx.doi.org/10.1039/c3md00161j |
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