In the next years, improvement of human quality of life thought more efficient and environmentally safety food production will be a challenge. Within this aim, the use of pesticides will continue, but rigorous testing and severer rules will shift research to find safer alternatives. To contribute for the discovery and development of new insecticides and as a continuation of our recent research interests in biopesticides, a series of eugenol esters derivatives were synthesized and evaluated for their insecticidal activities against the Sf9 cell line. In addition, a structured-based inverted virtual screening protocol was employed to identify the potential proteins associated to the observed insecticidal activity. The encouraging results obtained allowed to establish a preliminary structure-activity relationship.