Discovery of selective aminothiazole aurora kinase inhibitors.

  title={Discovery of selective aminothiazole aurora kinase inhibitors.},
  author={Carsten Juel Andersen and Yongqin Wan and Jae Won Chang and Blake Riggs and Christian Lee and Yi Liu and Fabio Sessa and Fabrizio Villa and Nicholas P. Kwiatkowski and Melissa Suzuki and Laxman Nallan and Rebecca Heald and Andrea Musacchio and Nathanael S Gray},
  journal={ACS chemical biology},
  volume={3 3},
Aurora family kinases regulate important events during mitosis including centrosome maturation and separation, mitotic spindle assembly, and chromosome segregation. Misregulation of Aurora kinases due to genetic amplification and protein overexpression results in aneuploidy and may contribute to tumorigenesis. Here we report the discovery of new small molecule aminothiazole inhibitors of Aurora kinases with exceptional kinase selectivity and report a 1.7 A cocrystal structure with the Aurora B… CONTINUE READING
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