This third edition of Medicinal Chemistry of Anticancer Drugs, provides an updated resource for students and researchers from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. This new edition includes updated sections on the hot topic of cancer immunotherapy, cancer polypharmacology, multitargeted cancer therapy, medicinal chemistry of cancer diagnosis, theranostic anticancer agents, and pre-mRNA processing in cancer. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a unique and valuable perspective from the point of view of medicinal chemistry and drug design. It will be useful to undergraduate and postgraduate students of medicinal chemistry, pharmacology, biological chemistry, pharmacy and other health sciences. Researchers and practitioners will find a comprehensive treatment of the topic and a large number of references to reviews and the primary literature.