Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 56, Issue 1, Pages 276-292Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm301593r
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Funding
- National Natural Science Foundation of China [90713038, 21072231]
- National Major Science and Technology Project of China [2009ZX09501-003, 2010ZX09401-401]
- 863 Program of China [2012AA020301]
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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 D-7.4, 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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