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Synthesis and antitumor activity evaluation of novel ursolic acid derivatives

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Eleven novel ursolic acid (UA) derivatives were designed and synthesized with modification at positions of C-2, C-3, and C-28 of UA. Their structures were confirmed by MS, 1H NMR, and elemental analysis. Their in vitro cytotoxicities against various cancer cell lines (HeLa, HepG2, and BGC-823) were evaluated by MTT assay. The results indicated that all compounds could inhibit cell proliferation of HeLa, HepG2, and BGC-823 cells. Among them, compounds I 3 and I 4 showed more potent cytotoxicity on these three tumor cells than gefitinib (positive control), worthy to be studied further.

Keywords: antitumor activity; synthesized; triterpenoid; ursolic acid derivatives

Document Type: Research Article

Affiliations: Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang, 110142, China

Publication date: 03 March 2016

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