In conclusion, by using both an in vitro and an in vivo approach, we showed that the newly synthetized phenolic compound AIF-1 is a potent ABCB1 modulator, as it inhibits the ABCB1-mediated resistance in NSCLC cells by increasing intracellular doxorubicin concentration and cancer-cell sensitivity to its toxicity. The gene discussed is ABCB1; the disease is cancer.