To investigate the antitumor activities of xanthonic compounds, 10 prenylated xanthone derivatives 2-11 along
with their key building block 1,3,6-trihydroxyxanthone 1 were evaluated for their potential cytotoxic activities against
HeLa and MDA-MB-231 cancer cell lines. The synthesis afforded a series of prenylated derivatives with typical and new
xanthone skeletons. Compounds 2, 3, 4 and 9 were reported for the first time to possess a new scaffold of 2H-xanthene-
3,9-dione. Interestingly, analogues 2 and 3 with the new scaffold demonstrated remarkable in vitro growth inhibitory
activities against both the cell lines by displaying a greater cytotoxic potency than the standard drugs used in the assay,
namely doxorubicin and cisplatin. In contrast, a dramatic loss of activity was observed for the O-prenylated derivatives 9-
11. These findings have highlighted the therapeutic potential of 2H-xanthene-3,9-dione scaffold to be exploitable as drug
lead with specific activity against cervical and breast cancers.
Keywords: 2H-xanthene-3, 9-dione scaffold, antiproliferation, antitumor agent, cytotoxicity, synthesis, xanthone derivatives, cervical, breast cancers, cancer cell lines, O-prenylated.
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Published on: 06 September, 2012
Page: [549 - 555]