2. Academic Validation
  3. 2-Aminobenzimidazoles as potent Aurora kinase inhibitors

2-Aminobenzimidazoles as potent Aurora kinase inhibitors

  • Bioorg Med Chem Lett. 2009 Sep 1;19(17):5158-61. doi: 10.1016/j.bmcl.2009.07.016.
Min Zhong 1,  Minna Bui,  Wang Shen,  Subramanian Baskaran,  Darin A Allen,  Robert A Elling,  W Michael Flanagan,  Amy D Fung,  Emily J Hanan,  Shannon O Harris,  Stacey A Heumann,  Ute Hoch,  Sheryl N Ivy,  Jeffrey W Jacobs,  Stuart Lam,  Heman Lee,  Robert S McDowell,  Johan D Oslob,  Hans E Purkey,  Michael J Romanowski,  Jeffrey A Silverman,  Bradley T Tangonan,  Pietro Taverna,  Wenjin Yang,  Josh C Yoburn,  Chul H Yu,  Kristin M Zimmerman,  Tom O'Brien,  Willard Lew
Affiliations

Affiliation

  • 1 Sunesis Pharmaceuticals, Inc., 395 Oyster Point Blvd., South San Francisco, CA 94080, USA. mzhong@presidiopharma.com
PMID: 19646866 DOI: 10.1016/j.bmcl.2009.07.016
Abstract

This Letter describes the discovery and key structure-activity relationship (SAR) of a series of 2-aminobenzimidazoles as potent Aurora Kinase inhibitors. 2-Aminobenzimidazole serves as a bioisostere of the biaryl urea residue of SNS-314 (1c), which is a potent Aurora Kinase Inhibitor and entered clinical testing in patients with solid tumors. Compared to SNS-314, this series of compounds offers better aqueous solubility while retaining comparable in vitro potency in biochemical and cell-based assays; in particular, 6m has also demonstrated a comparable mouse iv PK profile to SNS-314.

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