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

…, G Georges, RA Engh, B Goller…

Index: Rawson, Thomas E.; Rueth, Matthias; Blackwood, Elizabeth; Burdick, Dan; Corson, Laura; Dotson, Jenna; Drummond, Jason; Fields, Carter; Georges, Guy J.; Goller, Bernhard; Halladay, Jason; Hunsaker, Thomas; Kleinheinz, Tracy; Krell, Hans-Willi; Li, Jun; Liang, Jun; Limberg, Anja; McNutt, Angela; Moffat, John; Phillips, Gail; Ran, Yingqing; Safina, Brian; Ultsch, Mark; Walker, Leslie; Wiesmann, Christian; Zhang, Birong; Zhou, Aihe; Zhu, Bing-Yan; Rueger, Petra; Cochran, Andrea G. Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4465 - 4475

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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