期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 9, 页码 2062-2065出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.03.047
关键词
Xanthone; alpha-Mangostin; Anti-cancer agent; Cytotoxicity; Kinetic solubility
资金
- Gachon University research fund [GCU-2012-M065]
A xanthone-derived natural product, alpha-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. (C) 2014 Elsevier Ltd. All rights reserved.
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