Abstract
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 language | English |
|---|---|
| Pages (from-to) | 321-356 |
| Number of pages | 36 |
| Journal | Expert Opinion on Therapeutic Patents |
| Volume | 19 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - 2009 Mar 1 |
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All Science Journal Classification (ASJC) codes
- Pharmacology
- Drug Discovery
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Advances in Aurora kinase inhibitor patents. / Coumar, Mohane Selvaraj; Cheung, Chun-Hei; Chang, Jang-Yang; Hsieh, Hsing Pang.
In: Expert Opinion on Therapeutic Patents, Vol. 19, No. 3, 01.03.2009, p. 321-356.Research output: Contribution to journal › Review article
TY - JOUR
T1 - Advances in Aurora kinase inhibitor patents
AU - Coumar, Mohane Selvaraj
AU - Cheung, Chun-Hei
AU - Chang, Jang-Yang
AU - Hsieh, Hsing Pang
PY - 2009/3/1
Y1 - 2009/3/1
N2 - 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.
AB - 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.
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UR - http://www.scopus.com/inward/citedby.url?scp=67649408925&partnerID=8YFLogxK
U2 - 10.1517/13543770802646949
DO - 10.1517/13543770802646949
M3 - Review article
C2 - 19441907
AN - SCOPUS:67649408925
VL - 19
SP - 321
EP - 356
JO - Expert Opinion on Therapeutic Patents
JF - Expert Opinion on Therapeutic Patents
SN - 1354-3776
IS - 3
ER -