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...

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Main Authors: 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
Format: Artigo
Language:Inglês
Published: American Chemical Society 2012
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC3483018/
https://ncbi.nlm.nih.gov/pubmed/23043539
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300952s
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