Rongshi Li, PhD, is an Associate Professor in the Drug Discovery Department at H. Lee Moffitt Cancer Center and Research Institute in Tampa, Florida. Jeffrey A. Stafford, PhD, has led drug discovery research at GlaxoSmithKline, Syrrx, and Takeda. He is a co-inventor of the tyrosine kinase inhibitor, pazopanib (Armala).

• Preface ixContributors xiiiPart I Growth Factor Inhibitors: Vegfr2, Erbb2, And other Kinases 11 Discovery and Development of Sunitinib (SU11248): A Multitarget Tyrosine Kinase Inhibitor of Tumor Growth, Survival, and Angiogenesis 3Connie L. Sun, James G. Christensen, and Gerald McMahon2 Tykerb Discovery: A Dual EGFR and ERBB2 Tyrosine Kinase Inhibitor 41Karen Lackey and G. Stuart Cockerill Copyrighted Material3 Discovery of Pazopanib: A Pan Vascular Endothelial Growth Factor Kinase Inhibitor 57Philip A. Harris and Jeffrey A. Stafford4 Road to ABT-869: A Multitargeted Receptor Tyrosine Kinase Inhibitor 79Michael Michaelides and Daniel H. Albert5 Discovery of Motesanib 113Andrew S. Tasker and Vinod F. Patel6 Discovery of Brivanib Alaninate: A Dual Vascular Endothelial Growth Factor and Fibroblast Growth Factor Receptor Inhibitor 131Rajeev S. Bhide and Joseph Fargnoli7 Structure-Based Design and Characterization of Axitinib 167Robert S. KaniaPart II Growth Factor Inhibitors: Mek Inhibitors 2038 Road to PD0325901 and Beyond: The MEK Inhibitor Quest 205Judith S. Sebolt-Leopold and Alexander J. Bridges9 Discovery of Allosteric MEK Inhibitors 229Eli Wallace and James F. BlakePart III Cell Cycle Kinase Inhibitors: Aurora Kinase and Plk Inhibitors 25310 Discovery of MK-0457 (VX-680) 255Julian M. C. Golec11 Discovery of PHA-739358 281Daniele Fancelli and Jürgen Moll12 Discovery of AZD1152: A Selective Inhibitor of Aurora-B Kinase with Potent Antitumor Activity 309Kevin M. Foote and Andrew A. Mortlock13 Case Study of Aurora-A Inhibitor MLN8054 333Christopher F. Claiborne and Mark G. Manfredi14 Discovery of GSK461364: A Polo-like Kinase 1 Inhibitor for the Treatment of Cancer 351Kevin W. Kuntz and Kyle A. EmmittePart IV Related Special Topics 36515 Pharmacogenomics of Dasatinib (Sprycel TM) 367Fei Huang and Edwin A. Clark16 Practical Use of Computational Chemistry in Kinase Drug Discovery 403James M. Veal17 Approaches to Kinase Homology Modeling: Successes and Considerations for the Structural Kinome 433Victoria A. Feher and J. David Lawson18 Fragment-Based Drug Discovery of Kinase Inhibitors 461Daniel A. Erlanson19 Protein Kinase Structural Biology: Methods and Strategies for Targeted Drug Discovery 485Clifford D. Mol, Kengo Okada, and David J. HosfieldIndex 501

"In conclusion, I strongly recommend this book to anyone who is interested and new to the field of kinase inhibitors. Indeed, I believe this book should not merely sit on the shelves of kinase experts, but should be used frequently for reference." (ChemMedChem, 2010) "Delivers what the title promises: a comprehensive treatment of drugs that inhibit kinases. ... Will be interesting to any chemist or biologist desiring a behind-the-scenes look at modern strategies of drug discovery and their practical applications to some challenging targets." (Journal of Medicinal Chemistry, April 2010)