Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase

…, W von der Saal, A Limberg, G Georges…

Index: 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, 2011 , vol. 54, # 1 p. 312 - 319

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Citation Number: 39

Abstract

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) ...