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Prime, Michael E; Courtney, Stephen M; Brookfield, Frederick A; Marston, Richard W; Walker, Victoria; Warne, Justin; Boyd, Andrew E; Kairies, Norman A; von der Saal, Wolfgang; Limberg, Anja; Georges, Guy; Engh, Richard A; Goller, Bernhard; Rueger, Petra; Rueth, Matthias
Journal of medicinal chemistry, 01/2011, Letnik: 54, Številka: 1Journal Article
The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells has generated significant discussion within the literature. We report a novel class of Aurora kinase inhibitors based upon a phthalazinone pyrazole scaffold. The development of the phthalazinone template resulted in a potent Aurora-A selective series of compounds (typically >1000-fold selectivity over Aurora-B) that display good pharmacological profiles with significantly improved oral bioavailability compared to the well studied Aurora inhibitor VX-680.
