Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors

  • Bioorg Med Chem Lett. 2008 Oct 1;18(19):5186-9. doi: 10.1016/j.bmcl.2008.08.091.
Emily J Hanan  1 ,  Raymond V Fucini ,  Michael J Romanowski ,  Robert A Elling ,  Willard Lew ,  Hans E Purkey ,  Erica C VanderPorten ,  Wenjin Yang
Affiliations
  • 1. Sunesis Pharmaceuticals, Inc., 395 Oyster Point Boulevard Suite 400, South San Francisco, CA 94080, USA. [email protected]
PMID: 18790636 DOI: 10.1016/j.bmcl.2008.08.091
Abstract

A series of 2-amino-isoxazolopyridines was designed and synthesized as Polo-like kinase (PLK) inhibitors. Key SAR and crystallographic data are discussed. More advanced analogues inhibit PLK1 with good enzymatic activity and modest cell-based activity. Differential selectivity among the three PLK isoforms is observed.

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