Abstract A xanthone-derived natural product, α-mangostin is isolated from various parts of the mangosteen, Garcinia mangostana L.(Clusiaceae), a well-known tropical fruit. Novel xanthone derivatives based on α-mangostin were synthesized and evaluated as anti-cancer agents by cytotoxicity activity screening using 5 human cancer cell lines. Some of these analogs had potent to moderate inhibitory activities. The structure–activity relationship ...