Molecular medicines will continue to play a critical role in the treatment and diagnosis of cancer for the foreseeable future. The ability to build (synthesize) complex molecules is to be able to create structural and functional exclusivity, including new lead compounds for drug discovery and unique molecular research tools. We focus on the synthesis of targets with semivalidated anticancer activity and work collaboratively to understand and optimize this activity to our advantage. Our interest is piqued by small molecule natural products that induce phenotypic-, pathway-, or target-specific activity. Recently, our interest has been focused on molecules that cause autophagy, activate novel apoptosis-induction pathways, and bind to important biomolecules such as actin or the proteasome. Sometimes a natural substance will act in new ways on cancer cells and thereby represent the opportunity to discover novel approaches to managing disease. We place a premium on developing innovative methods and strategies towards the synthesis of complex molecules with provocative anticancer function. We are at our best as part of a collaborative research program where our synthetic capability creates exclusive access to molecular tools that enable us to register advances in understanding and in contributing to the treatment of cancer.