Synthesis And Bioevaluation Of Novel Oxa-Caged Garcinia Xanthones As Anti-Tumour Agents
AUSTRALIAN JOURNAL OF CHEMISTRY（2015）
摘要
Gambogic acid (GA), a special category of Garcinia xanthones, has attracted great attention owing to its striking bioactivities and unique structure. To further explore its structure-activity relationship, we prepared seven novel oxa-caged Garcinia xanthones that were for the first time varied at the C-2 position of B ring and at the C-21/22 or C-23 position of the prenyl group in the caged scaffold. Some compounds exhibited strong anti-proliferation activities in different cancer cell lines. Particularly, compound 8 showed more potent cytotoxic activity and better selectivity towards the A549 cell line than GA. Oxa-caged xanthones 8 was identified as an A549 cell apoptosis inducer through observations of morphological changes and Annexin-V/PI double-staining assay. Additionally, the structure-activity relationships of these new analogues were discussed.
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关键词
interfaces,peptide,medicinal chemistry,polymer chemistry,ab initio calculations,quantum chemistry,colloids,biological chemistry,educational,nanotechnology,structure,inorganic chemistry,sensors,amino acids,surface chemistry,proteins,organic chemistry,ionic liquids,biocatalysis,enzymes,pharmaceutical chemistry,computational chemistry,macromolecules,combinatorial chemistry,green chemistry,combinatorial,self assembly,crystal structures,reaction mechanisms,photochemistry,crystallography,electrochemistry,catalysis,supramolecular chemistry,kinetics,mass spectrometry,analytical chemistry,spectroscopy,biosensors,density functional theory,physical chemistry
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