Accumulating evidence has shown the crucial role of the caspase family in both initiation and regulation of apoptosis. Caspases-3 and -7 are at the core of the execution phase of apoptosis. Like most proteases, these “executioner” caspases are stored as procaspases that once activated by proteolysis cleave a large set of substrates, ultimately resulting in the characteristic morphological and biochemical hallmarks of apoptosis. Therefore, the search for activators of these procaspases has deserved particular attention in the field of anticancer drug discovery. Nevertheless, to date, only a few small-molecule these activators of caspases have been reported.