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

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

  • Bioorg Med Chem Lett. 2014 May 1;24(9):2062-5. doi: 10.1016/j.bmcl.2014.03.047.
Xiang Fei 1,  Minmi Jo 2,  Bit Lee 1,  Sang-Bae Han 3,  Kiho Lee 2,  Jae-Kyung Jung 3,  Seung-Yong Seo 4,  Young-Shin Kwak 5
Affiliations

Affiliations

  • 1 College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon 406-779, Republic of Korea.
  • 2 College of Pharmacy, Korea University, Sejong 339-700, Republic of Korea.
  • 3 College of Pharmacy and Medicinal Research Center (MRC), Chungbuk National University, Cheongju 361-763, Republic of Korea.
  • 4 College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon 406-779, Republic of Korea. Electronic address: syseo@gachon.ac.kr.
  • 5 College of Pharmacy, Korea University, Sejong 339-700, Republic of Korea. Electronic address: youngshin@korea.ac.kr.
PMID: 24717154 DOI: 10.1016/j.bmcl.2014.03.047
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.

Keywords

Anti-cancer agent; Cytotoxicity; Kinetic solubility; Xanthone; α-Mangostin.

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