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Synthesis of xanthone derivatives based on alpha-mangostin and their biological evaluation for anti-cancer agents

Authors
Fei, XiangJo, MinmiLee, BitHan, Sang-BaeLee, KihoJung, Jae-KyungSeo, Seung-YongKwak, Young-Shin
Issue Date
1-May-2014
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Xanthone; alpha-Mangostin; Anti-cancer agent; Cytotoxicity; Kinetic solubility
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.24, no.9, pp.2062 - 2065
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
24
Number
9
Start Page
2062
End Page
2065
URI
https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/12634
DOI
10.1016/j.bmcl.2014.03.047
ISSN
0960-894X
Abstract
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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