Synthesis and anti-tumor activity of asiatic acid derivatives targeting VEGFR

Abstract

To discovery novel VEGFR inhibitors, 12 novel asiatic acid derivatives were designed by computer-aided drug design (CADD) technology. Then, these novel asiatic acid derivatives were synthesized by introducing active groups at ring A and C-28 positions of asiatic acid. The structures of these novel analogues were confirmed by NMR and MS. Moreover, the anti-tumor activities of these novel asiatic acid derivatives on human hepatoma cells HepG2 and human gastric cancer cells SGC7901 were evaluated by MTT assay. As a result, compounds I₂ and II₄ showed stronger cytotoxicity on tumor cells than asiatic acid and positive control drugs such as gefitinib and paclitaxel. In conclusion, our study synthesized twelve novel asiatic acid derivatives and determined compounds I₂ and II₄ had better anti-tumor effect which may be potential candidate compounds for tumor therapy.

Keywords:

• Asiatic acid derivatives
• molecular docking
• anti-tumor activity

Disclosure statement

No potential conflict of interest was reported by the author(s).

Correction Statement

This article has been corrected with minor changes. These changes do not impact the academic content of the article.

Additional information

Funding

This work was financially supported by National Natural Science Foundation of China [21372156], the Liaoning Province Key Research & Development project [2019JH2/10300034], the Key Project of Education Department of Liaoning Province [LJKZ0427], the Project of Education Department of Liaoning Province [LJKZ0427], the Shenyang Major Scientific and Technological Achievement Transformation Project [20-203-5-45], the Key Research and Local Service Project of Shenyang University of Chemical Technology [LDB2019001].