Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592579 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
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 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.
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Authors
Xiang Fei, Minmi Jo, Bit Lee, Sang-Bae Han, Kiho Lee, Jae-Kyung Jung, Seung-Yong Seo, Young-Shin Kwak,