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This lecture covers the basics of drug discovery and development, focusing on small molecule drugs for cancer treatment. It delves into the molecular and chemical basis of cancer, the mechanisms of action of anti-cancer drugs, and the historical development of early anti-cancer agents. The instructor discusses the importance of understanding drug targets, major diseases, and the different classes of anti-cancer drugs. Specific topics include alkylating agents, antimetabolites, monoclonal antibodies, and signal transduction inhibitors. Case studies and examples such as Glivec and paclitaxel are used to illustrate the rational design and targeted approach in developing anti-cancer therapies.