1;Volume Editor;5 2;Editorial Board;5 3;Topics in Medicinal Chemistry Also Available Electronically;6 4;Preface to the Series;7 5;Preface to Volume 1;8 6;Contents;10 7;Overview;12 7.1;1 Introduction;13 7.2;2 Historical Perspective;13 7.3;3 Cytotoxic Drugs;14 7.4;4 Anti-hormonal Drugs;16 7.5;5 Targeted Drugs;17 7.6;6 Structure of This Volume;23 7.7;7 Conclusion;25 7.8;References;25 8;Anti-hormone Therapy: Principles of EndocrineTherapy of Cancer;30 8.1;1 Introduction;32 8.2;2 Chemistry and Pharmacology of Endocrine Therapy;45 8.3;3 Conclusion and Outlook;84 8.4;References;85 9;Inhibition of Growth Factor Signaling by Small- Molecule Inhibitors of ErbB, Raf, and MEK;94 9.1;1 Introduction;96 9.2;2 Biological Background and Rationale;96 9.3;3 Structural Biology;99 9.4;4 Inhibitors of the ErbB Family;106 9.5;5 Inhibitors of Raf;124 9.6;6 Inhibitors of MEK;128 9.7;7 Biomarkers;132 9.8;8 Conclusions and Outlook;135 9.9;References;137 10;Farnesyl Protein Transferase Inhibitors: Medicinal Chemistry, MolecularMechanisms, and Progress in the Clinic;144 10.1;1 Introduction and Historical Overview;146 10.2;2 Biochemistry of Farnesyl Protein Transferase;147 10.3;3 Downstream Effectors;149 10.4;4 Biomarkers;157 10.5;5 Farnesyl Transferase Inhibitors;158 10.6;6 Clinical Experience;168 10.7;7 Further Developments;168 10.8;8 Conclusion and Perspectives;170 10.9;References;171 11;Survival Signaling;180 11.1;1 Introduction;182 11.2;2 Insulin-like Growth Factor I Receptor;183 11.3;3 Phosphatidylinositol 3-Kinases;189 11.4;4 3-Phosphoinositide-dependent Protein Kinase-1;194 11.5;5 Protein Kinase B;197 11.6;6 Mammalian Target of Rapamycin;201 11.7;7 Other Medicinal Chemistry Approaches to Block the Survival Pathway;203 11.8;8 PI3K/PKB Pathway Modulators with Unknown Mechanism of Action;208 11.9;9 Conclusions and Outlook;210 11.10;References;211 12;Progress in the Development of Agents to Control the Cell Cycle;218 12.1;1 Introduction;220 12.2;2 Cyclin-Dependent Kinases;220 12.3;3 Aurora Kinases;262 12.4;4 Polo-Like Kinases;280 12.5;5 Conclusion;291 12.6;References;292 13;HDAC Inhibition in Cancer Therapy: An Increasingly Intriguing Tale of Chemistry, Biology and Clinical Benefit;304 13.1;1 Introduction;306 13.2;2 Biochemistry of the Histone Deacetylases and Histone Acetyl Transferases;307 13.3;3 HDAC Inhibitors;311 13.4;4 Clinical Experience with HDAC Inhibitors;328 13.5;5 Perspectives and Conclusion;335 13.6;References;337 14;Development of Angiogenesis Inhibitors to Vascular Endothelial Growth Factor Receptor 2 for Cancer Therapy;344 14.1;1 Introduction;346 14.2;2 Vascular Endothelial Growth Factor and Its Receptors;346 14.3;3 Vascular Endothelial Growth Factor Receptor-2;348 14.4;4 Future Perspective;379 14.5;References;380 15;Novel Small-Molecule Inhibitors of Src Kinase for Cancer Therapy;394 15.1;1 Introduction;395 15.2;2 Src Kinase Genetics and Signal Transduction;397 15.3;3 Src Kinase Inhibitor: Structural Biology and Drug Design;399 15.4;4 Src Kinase Inhibitor: Chemical Diversity and Biological Properties;402 15.5;5 Src Kinase Inhibitor: Drug Development for Cancer Therapy;410 15.6;6 Concluding Remarks;410 15.7;References;411 16;Bcr-Abl Kinase Inhibitors;418 16.1;1 Bcr-Abl: The Hallmark of Chronic Myelogenous Leukemia (CML);419 16.2;2 Imatinib, a Bcr-Abl Kinase Inhibitor Effective in Treating CML;420 16.3;3 New Bcr-Abl Kinase Inhibitors;422 16.4;4 Dual Inhibitors of Bcr-Abl and Src Kinases;429 16.5;5 Key Issues;443 16.6;6 Present Status and Future Outlook;446 16.7;References;448 17;Author Index Volume 1;456 18;Subject Index;458