Synthesis and antitumor activity evaluation of novel ursolic acid derivatives

Abstract

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 I₃ and I₄ showed more potent cytotoxicity on these three tumor cells than gefitinib (positive control), worthy to be studied further.

Keywords:

• ursolic acid derivatives
• triterpenoid
• synthesized
• antitumor activity

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by the Natural Science Foundation of China [No. 21372156], Program for Liaoning Excellent Talents in University [No. LR2013017], Program of Science and Technology in Shenyang of China [No. F13-316-1-47].