Research directions for new therapies in oncology are shifting from purely cytotoxic or cytostatic agents to enzyme inhibitors targeting signaling pathways, as well as agents that are preferentially absorbed by cancer cells or influence vascularization and tissue adhesion or penetration. Natural products continue to be of great utility as biological tools as well as therapeutic agents, and the diversity of natural structures continues to impress and inspire medicinal chemistry. Increased recognition is also given to diversity-oriented synthesis, which aspires to mimic the structural wealth and three-dimensional architectures of natural products.