A Class of 2, 4-Bisanilinopyrimidine Aurora A Inhibitors with Unusually High Selectivity against Aurora B†

I Aliagas-Martin, D Burdick, L Corson…

文献索引：Aliagas-Martin, Ignacio; Burdick, Dan; Corson, Laura; Dotson, Jennafer; Drummond, Jason; Fields, Carter; Huang, Oscar W.; Hunsaker, Thomas; Kleinheinz, Tracy; Krueger, Elaine; Liang, Jun; Moffat, John; Phillips, Gail; Pulk, Rebecca; Rawson, Thomas E.; Ultsch, Mark; Walker, Leslie; Wiesmann, Christian; Zhang, Birong; Zhu, Bing-Yan; Cochran, Andrea G. Journal of Medicinal Chemistry, 2009 , vol. 52, # 10 p. 3300 - 3307

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被引用次数: 64

摘要

The two major Aurora kinases carry out critical functions at distinct mitotic stages. Selective inhibitors of these kinases, as well as pan-Aurora inhibitors, show antitumor efficacy and are now under clinical investigation. However, the ATP-binding sites of Aurora A and Aurora B are virtually identical, and the structural basis for selective inhibition has therefore not been clear. We report here a class of bisanilinopyrimidine Aurora A inhibitors with excellent ...