Synthesis of xanthone derivatives based on alpha-mangostin and their biological evaluation for anti-cancer agents
- Authors
- Fei, Xiang; Jo, Minmi; Lee, Bit; Han, Sang-Bae; Lee, Kiho; Jung, Jae-Kyung; Seo, Seung-Yong; Kwak, 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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