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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Antitumor Activities of α-,γ-mangostin Derivatives

Author(s): Kai Cheng, Gui-lin Zhang, Sheng-xiang Qiu, Yan-qing Liu, Yan-fei Wang, Song Liu, Yan Shan, Bo Yu and Yu Lu

Volume 11 , Issue 5 , 2014

Page: [586 - 593] Pages: 8

DOI: 10.2174/1570180811666131217003216

Price: $65


The α-Mangostin and -Mangostin were mainly isolated from Garcinia Mangostana L. as representative Xanthone's natural products of plant origin, revealed high activity of antitumor, antioxidation and other diverse pharmacological activities. A series of α, γ-Mangostin derivatives LT-1~17 has been synthesized, and confirmed by 1H NMR, 13C NMR, MS(supplement file). Compounds LT-2~17, as novel Xanthone, have been reported for the first time. Their antitumor activities have been investigated by MTT method in cell lines: A549, K562, CNE, KB-3-1, MCF-7 and HepG2. A number of compounds showed potent anti-tumor activity, in some cases even higher (more effective) than Mangostins. Compound 3 with an IC50 value of 1.73 µM in the A549 cell line, which was two-fold, acted more active than ADM (adriamycin) and α, γ-Mangostin, and had the most potent anti-tumor activity (IC50=2.15 µM) for the MCF-7 cell line in all synthetic derivatives. α, γ-Mangostin and ADM showed potent anti-tumor activity (IC50=2.82 µM) for HepG2 cell line, and less potent anti-tumor activity in other cell lines compared with the compound LT-12. It was obtained by esterification of the C-3, C-7 phenolic-OH of the α-Mangostin with acetyl group resulted the potent anti-tumor acvitity, which indicated that the phenolic-OH of the Mangostins had a great impaction on the anti-tumor activity of Mangostins.

Keywords: Anticancer drugs, α, γ-mangostin derivatives, Xanthone, Pharmacological activity.

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