Caspases-3 and -7 play a key role in the activation of apoptosis, and therefore the search for activators of these proteases has therefore deserved particular attention in the field of antineoplasic drug discovery. This work describes the implementation of a screening system for activators of these human caspases based on yeast, a unicellular eukaryotic organism, as a simplified cell model for large-scale research. Using this approach we identified two new potential activators of caspase-7, which did not interfere with the activity of caspase-3 in yeast.