Tormentic acid derivatives: Synthesis and apoptotic activity

Several derivatives of tormentic acid have been prepared and tested for their antitumor activity. The dichloroacetate 14 is an excellent antitumor active agent acting by an apoptose inducing pathway as demonstrated by OA/PI staining, DNA laddering experiments as well as by an annexin V binding assay.

Graphical abstractSeveral tormentic acid derivatives show a significant antitumor activity. The most active compound of this series showed an average IC50 value of 1.3 μmol; it acts by apoptosis as shown by a dye exclusion test, an extra acridine orange/propidium bromide staining, an annexin V assay and DNA laddering experiments.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► In this study we synthesized and investigate acylated tormentic acid derivatives. ► The compounds were tested for their antitumor activity using 7 different human cancer cell lines. ► Several derivatives are cytotoxic; one of them in a low μmol concentration. ► The compounds act by apoptosis.