Advances in Aurora kinase inhibitor patents

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

Research output: Contribution to journalReview articlepeer-review

24 Citations (Scopus)


Background: Aurora-A, Aurora-B and Aurora-C, members of serine/threonine kinase family, play an important role in mitosis. They are essential for spindle assembly, centrosome maturation, chromosomal segregation and cytokinesis during mitosis. Abnormalities in the mitotic process as a result of overexpression/amplification of Aurora kinase have been linked to genomic instability leading to tumorigenesis. Hence, the use of Aurora kinase small-molecule inhibitors as a potential molecular-targeted therapeutic intervention for cancer is being pursued. Objective: A number of reviews focus on the biology of Aurora kinase; a few focus on the medicinal chemistry aspect of Aurora kinase inhibitor development. Here, we review the medicinal chemistry aspect of Aurora kinase inhibitors, with a particular emphasis on the patent literature. Method: The Scifinder® and Delphion® databases were used to search the literature for Aurora kinase inhibitors. Approximately 150 patents and 700 journal references are available, most of them published in the last 5 years. Conclusion/results: Analysis of the literature reveals three common strategies utilized by different groups in developing Aurora kinase inhibitors. These are discussed in detail and could be of use to medicinal chemists in laying out new strategies for developing novel Aurora kinase inhibitors.

Original languageEnglish
Pages (from-to)321-356
Number of pages36
JournalExpert Opinion on Therapeutic Patents
Issue number3
Publication statusPublished - 2009 Mar

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery


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