Aurora kinase inhibitor patents and agents in clinical testing: An update (2009 - 10)

Chun Hei Antonio Cheung, Mohane Selvaraj Coumar, Jang Yang Chang, Hsing Pang Hsieh

Research output: Contribution to journalReview articlepeer-review

42 Citations (Scopus)


Introduction: Mitosis is a key step in the cell cycle and is controlled by several cell cycle regulators, including aurora kinases. Aurora family members A, B and C are essential for spindle assembly, centrosome maturation, chromosomal segregation and cytokinesis. Overexpression/amplification of aurora kinases has been implicated in oncogenic transformation, including the development of chromosomal instability in cancer cells. Hence, the use of aurora kinase small molecule inhibitors as a potential molecular-targeted therapeutic intervention for cancer is being pursued by various researchers. Area covered: This review provides an update on aurora kinase inhibitors based on developments from 2009 to 2010. The medicinal chemistry aspects of aurora kinase inhibitors, with a particular emphasis on the patent literature, are reviewed. Databases such as PubMed, SCOPUS, Scifinder and database were used to search for literature in the preparation of this review. Expert opinion: Around a dozen aurora kinase inhibitors are currently undergoing various Phase I - II evaluations for different human cancers. Instead of being applied as a monotherapy, combinations of aurora kinase inhibitors and existing chemotherapeutic compounds seem to give better therapeutic outcomes and are, therefore, a promising future cancer therapy.

Original languageEnglish
Pages (from-to)857-884
Number of pages28
JournalExpert Opinion on Therapeutic Patents
Issue number6
Publication statusPublished - Jun 2011
Externally publishedYes


  • AMG 900
  • AT-9283
  • aurora kinase inhibitors
  • AZD1152
  • BI811283
  • CYC116
  • ENMD-2076
  • GSK1070916
  • MLN8054
  • MLN8237
  • PF-3814735
  • PHA739358
  • R763
  • SNS-314
  • VX-680/MK0457
  • VX-689/MK-5108
  • XL228

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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