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

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.

• Authors: Xiang Fei, Minmi Jo, Bit Lee, Sang-Bae Han, Kiho Lee, Jae-Kyung Jung, Seung-Yong Seo, Young-Shin Kwak
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 24 Issue 9 Pg. 2062-5 (May 01 2014) ISSN: 1464-3405 [Electronic] England
• PMID: 24717154 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2014 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents, Phytogenic
• Xanthones
• mangostin

Topics

• Antineoplastic Agents, Phytogenic (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Garcinia mangostana (chemistry)
• Humans
• Neoplasms (drug therapy)
• Structure-Activity Relationship
• Xanthones (chemical synthesis, chemistry, pharmacology)