A xanthone-derived natural product, a-mangostin is isolated from various parts of the mangosteen,
Garcinia mangostana L. (Clusiaceae), a well-known tropical fruit. Novel xanthone derivatives based on
a-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 studies revealed that phenol groups on C3 and C6 are critical to
anti-proliferative activity and C4 modification is capable to improve both anti-cancer activity and
drug-like properties. Our findings provide new possibilities for further explorations to improve potency.