Synthesis and antitumor activity evaluation of new asiatic acid derivatives

Abstract

Twelve novel asiatic acid (AA) derivatives were designed and synthesized. Their structures were confirmed using NMR, MS, and IR spectra. Their in vitro cytotoxicities on various cancer cell lines (HeLa, HepG2, BGC-823, and SKOV3) were evaluated by the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay. Most of the derivatives were found to have stronger cell growth inhibitory activity than AA. Among them, compounds 5–8 and 11 with substituted amide group at C-28 exhibited more potent cytotoxicity than AA, Gefitinib, and etoposide (positive control).