Schweinfurthin G, a stilbenoid, was originally identified and isolated from Macaranga alnifolia, which were also isolated from Macaranga tanarius growing in Vietnam in high yield. This compound exhibited a strong cytotoxicity against A549 and KB cell lines with the IC50 values of 0,80 μM and 0,6 μM, respectively. However, there are few papers reporting about total synthesis of this derivative. In this paper, we reported the synthesis of a new diamide derivative of schweinfurthin G from schweinfurthin G through six reaction steps and this compound exhibited a strong cytotoxicity against KB cancer cell line with an IC50 value of 4,4 μM.