MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
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- 作者：Todd B. Sells ; Ryan Chau ; Jeffrey A. Ecsedy ; Rachel E. Gershman ; Kara Hoar ; Jessica Huck ; David A. Janowick ; Vivek J. Kadambi ; Patrick J. LeRoy ; Matthew Stirling ; Stephen G. Stroud ; Tricia J. Vos ; Gabriel S. Weatherhead ; Deborah R. Wysong ; Mengkun Zhang ; Suresh K. Balani ; Joseph B. Bolen ; Mark G. Manfredi ; Christopher F. Claiborne
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2015
- 出版时间：June 11, 2015
- 年：2015
- 卷：6
- 期：6
- 页码：630-634
- 全文大小：254K
- ISSN：1948-5875
文摘
The Aurora kinases are essential for cell mitosis, and the dysregulation of Aurora A and B have been linked to the etiology of human cancers. Investigational agents MLN8054 (8) and alisertib (MLN8237, 10) have been identified as high affinity, selective, orally bioavailable inhibitors of Aurora A that have advanced into human clinical trials. Alisertib (10) is currently being evaluated in multiple Phase II and III clinical trials in hematological malignancies and solid tumors.