Mechanisms of in situ activation for DNA-targeting antitumor agents

o date, several well-established methods have been discovered or developed for in situ activation of antitumor agents in the presence of their molecular targets. Most have been discovered discovered through investigations of naturally occurring antitumor agents that defined the site and mechanisms of action and provided a detailed understanding of the structural origin of the properties. In addition to shape-dependent catalysis as it applies to CC-1065 and the duocarmycins, these methods enlist oxidation, reduction, nucleophilic attack, elimination, photochemical activation, and metal complexation of suitable precursors to generate reactive species near or at the site of action.