New drugs have been and will continue to be one of the most effective ways to fight cancer. Recent advances in cancer biology and genetics are ushering in a new era of drug discovery and treatment. Developing more effective and less toxic drug therapies that go after the novel targets revealed through basic science research is a primary goal. The Cancer Chemical and Structural Biology Program brings together faculty with strengths in cancer biology, chemistry, structural biology, engineering, pharmacology, and translation science to discover and validate new drug leads and to help turn them into new therapies. Investigators are discovering and testing new targets, improving the delivery and effectiveness of existing drug therapies, and exploring drug libraries of FDA-approved drugs for their potential to act against cancer. These discoveries are leading to therapies that interfere with biochemical pathways and molecular functions that cancer cells rely on to grow and spread, to assays that guide the right treatments to the right patients, and to sophisticated methods that more precisely get drugs into cancer cells while avoiding normal tissues. The efforts of the Cancer Chemical and Structural Biology Program serve as a hub for foundational and translational investigators to work together to develop and evaluate novel agents and molecular-based diagnostics for cancer.