This work aims to optimize the extraction of bioactive compounds with antiproliferative activity of goji berry (Lycium barbarum) and assess the extraction kinetic models. The extraction was performed by varying the proportion of ethanol:water solvent. The antioxidant activity determination tests indicated a significant difference for the proportion of 60:40 ethanol:water. Conditions of the highest levels of antioxidant activity at 45 °C and 6.71 min for ultrasound and at 45 °C and 23.30 h for shaker. The quantification of phenolic compounds, flavonoids, carotenoids, and anthocyanins showed that the ultrasound method led to the highest concentrations of these compounds. The extraction kinetics was evaluated, and the So and Mac Donald's and Second Order models showed the best fit, with a global maximum deviation lower than 10.0%. High concentrations of extracts produced showed cytotoxic effects for human hepatoma cells by the MTT test. The extract produced by Ultrasound reached cell viability of 37.71%.This article is protected by copyright. All rights reserved.