2. Academic Validation
  3. Discovery of a potent and selective aurora kinase inhibitor

Discovery of a potent and selective aurora kinase inhibitor

  • Bioorg Med Chem Lett. 2008 Sep 1;18(17):4880-4. doi: 10.1016/j.bmcl.2008.07.073.
Johan D Oslob 1,  Michael J Romanowski,  Darin A Allen,  Subramanian Baskaran,  Minna Bui,  Robert A Elling,  William M Flanagan,  Amy D Fung,  Emily J Hanan,  Shannon Harris,  Stacey A Heumann,  Ute Hoch,  Jeffrey W Jacobs,  Joni Lam,  Chris E Lawrence,  Robert S McDowell,  Michelle A Nannini,  Wang Shen,  Jeffrey A Silverman,  Michelle M Sopko,  Bradley T Tangonan,  Juli Teague,  Josh C Yoburn,  Chul H Yu,  Min Zhong,  Kristin M Zimmerman,  Tom O'Brien,  Willard Lew
Affiliations

Affiliation

  • 1 Medicinal Chemistry, Sunesis Pharmaceuticals, 395 Oyster Point Boulevard, South San Francisco, CA 94080, USA.
PMID: 18678489 DOI: 10.1016/j.bmcl.2008.07.073
Abstract

This communication describes the discovery of a novel series of Aurora Kinase inhibitors. Key SAR and critical binding elements are discussed. Some of the more advanced analogues potently inhibit cellular proliferation and induce phenotypes consistent with Aurora Kinase inhibition. In particular, compound 21 (SNS-314) is a potent and selective Aurora Kinase Inhibitor that exhibits significant activity in pre-clinical in vivo tumor models.

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