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.

doi:10.1021/jm300952s

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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.

Journal of medicinal chemistry - 25 Oct 2012

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

Abstract excerpt

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 nM, Aurora-B K(d) = 48 nM), FLT3 kinase (K(d) = 6.2 nM), and FLT3 mutants including FLT3-ITD (K(d) = 38 nM) and FLT3(D835Y) (K(d) =...

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PMID: 23043539
DOI: 10.1021/jm300952s
PMCID: PMC3483018

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FLT3

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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.PMID 23043539Read ↗

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