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J Med Chem. 2013 Jan 10;56(1):276-92. doi: 10.1021/jm301593r. Epub 2012 Dec 31.

Garcinia xanthones as orally active antitumor agents.

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State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.


Using a newly developed strategy whose key step is the regioselective propargylation of hydroxyxanthone substrates, 99 structurally diverse Garcinia natural-product-like xanthones based on gambogic acid were designed and synthesized and their in vitro antitumor activity was evaluated. A set of 40 related compounds was chosen for determination of their physicochemical properties including polar surface area, log Dā‚‡.ā‚„, aqueous solubility, and permeability at pH 7.4. In the light of the in vitro antitumor activity and the physicochemical properties, two compounds were advanced into in vivo efficacy experiments. The antitumor activity of compound 112, administered po, showed more potent in vivo oral antitumor activity than gambogic acid.

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