A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.

@article{AliagasMartin2009ACO,
  title={A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.},
  author={Ignacio Aliagas-Martin and Dan Burdick and Laura Corson and Jennafer Dotson and Jason Drummond and Carter T Fields and Oscar W. Huang and Thomas L. Hunsaker and Tracy L. Kleinheinz and Elaine Krueger and Jun Liang and John B. Moffat and Gail Phillips and Rebecca Pulk and Thomas E Rawson and Mark H. Ultsch and Leslie E. Walker and Christian Wiesmann and Birong Zhang and Bing-yan Zhu and Andrea G Cochran},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 10},
  pages={3300-7}
}
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 selectivity for Aurora A over… CONTINUE READING

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