880489-31-6Relevant articles and documents
Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase
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
, p. 312 - 319 (2011/03/20)
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.