Overview.- Anti-hormone Therapy: Principles of Endocrine Therapy of Cancer.- Inhibition of Growth Factor Signaling by Small-Molecule Inhibitors of ErbB, Raf, and MEK.- Farnesyl Protein Transferase Inhibitors: Medicinal Chemistry, Molecular Mechanisms, and Progress in the Clinic.- Survival Signaling.- Progress in the Development of Agents to Control the Cell Cycle.- HDAC Inhibition in Cancer Therapy: An Increasingly Intriguing Tale of Chemistry, Biology and Clinical Benefit.- Development of Angiogenesis Inhibitors to Vascular Endothelial Growth Factor Receptor 2 for Cancer Therapy.- Novel Small-Molecule Inhibitors of Src Kinase for Cancer Therapy.- Bcr-Abl Kinase Inhibitors.