Chapter 7. Structure-Based Design and Characterization of Axitinib
- Rongshi Li,
- Jeffrey A. Stafford
Published Online: 28 SEP 2009
DOI: 10.1002/9780470524961.ch7
Copyright © 2009 John Wiley & Sons, Inc.
Book Title
Kinase Inhibitor Drugs
Additional Information
How to Cite
Kania, R. S. (2009) Structure-Based Design and Characterization of Axitinib, in Kinase Inhibitor Drugs (eds R. Li and J. A. Stafford), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9780470524961.ch7
Editor Information
Takeda San Diego, Inc., San Diego, CA 92121, USA
Publication History
- Published Online: 28 SEP 2009
- Published Print: 2 OCT 2009
ISBN Information
Print ISBN: 9780470278291
Online ISBN: 9780470524961
- Summary
- Chapter
- References
Keywords:
- structure-based design and axitinib characterization;
- indazole series discovery;
- deep-pocket binders - amide functional group addition
Summary
This chapter contains sections titled:
Introduction
Project Underpinning
Lead Selection: Structures of HITS and of Proteins
Discovery of the Indazole Series
Targeting the DFG-Out Conformation
Extended 6-Linker Indazoles: Capturing all Efficient Interactions
Deep-Pocket Binders: Addition of an Amide Functional Group
Refinement and Characterization of the Deep-Pocket Binder Axitinib
Preclinical and Clinical Development of Axitinib
Summary
Acknowledgments
References