In order to explore structure-activity relationship (SAR) associated with xanthone framework, a series of prenylated xanthone derivatives 2-9 was synthesized from the key building block 1,3,6,8-tetrahydroxyxanthone 1 and evaluated for their in vitro growth inhibitory activities against HeLa and MDA-MB-231 human cancer cell lines. The in vitro evidence indicated that the inhibitory activity was significantly influenced by the position and number of linked group on the xanthone skeleton, and the presence of chroman-4-one moiety in the xanthone scaffold was found to be critically important for strong cytotoxic activity. The novel 2H-xanthene-3,9-dione analogues 3 and 4 were reported to elicit potent activities comparable to those of standard drugs doxorubicin and cisplatin. This preliminary investigation has highlighted the therapeutic potential of 2H-xanthene-3,9-dione derivatives to be exploitable as lead compound for the development of potent HeLa and MDA-MB-231 cancer cell inhibitors.
Keywords: Cytotoxicity, 2H-xanthene-3,9-dione scaffold, 2H-xanthene-3,6,9(7H)-trione scaffold, Inhibitory activity, Synthesis, Xanthone derivatives, SAR, Xanthone, HeLa, MDA-MB-231, Cancer, prenylated, anti-inflammatory, 1,3-dihydroxyxanthone, phloroglucinol, acylphloroglucinols
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