Synthesis and anti-tumor activity of derivatives of ursolic acid in vitro / 药学学报

ABSTRACT

A series of ursolic acid derivatives were synthesized by the introduction of 4-chloroindole compounds at A ring and esterification and amidation at C-28 position, which structures were characterized by 1H NMR, MS and etc. The cytotoxic activity of derivatives was evaluated against HepG2 and SGC7901 cells in vitro by MTT assay, in which paclitaxel and adriamycin were used as a positive control. The results indicated that all of derivatives can inhibit cell proliferation in HepG2 and SGC7901 cells with a better activity than ursolic acid. Especially, the compounds 6 and 12 showed significant antitumor activity comparable to the paclitaxel. The compounds are worthy to be studied further.