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Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia
[Image: see text] Optimization of the imidazo[4,5-b]pyridine-based series of Aurora kinase inhibitors led to the identification of 6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine (27e), a potent inhibitor of Aurora kinases (Aurora-A K(d) = 7.5...
Autores principales: | Bavetsias, Vassilios, Crumpler, Simon, Sun, Chongbo, Avery, Sian, Atrash, Butrus, Faisal, Amir, Moore, Andrew S., Kosmopoulou, Magda, Brown, Nathan, Sheldrake, Peter W., Bush, Katherine, Henley, Alan, Box, Gary, Valenti, Melanie, de Haven Brandon, Alexis, Raynaud, Florence I., Workman, Paul, Eccles, Suzanne A., Bayliss, Richard, Linardopoulos, Spiros, Blagg, Julian |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2012
|
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3483018/ https://www.ncbi.nlm.nih.gov/pubmed/23043539 http://dx.doi.org/10.1021/jm300952s |
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