2. Academic Validation
  3. Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors

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

Affiliation

  • 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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