Guanaconetins, new antitumoral acetogenins, mitochondrial complex I and tumor cell growth inhibitors

The antitumoral activity of a series of acetylated bis-tetrahydrofuranic acetogenins with a threo/trans/threo/trans/erythro relative configuration was characterized by four new natural and two semisynthetic, 15,24,30-trioxygenated acetogenins that were found to inhibit mitochondrial complex I enzyme as well as growth of several tumor cell lines. Placement of acetyl groups along the alkyl chain modulated the potency of the bis-tetrahydrofuranic acetogenins and could be important for future utilization of these compounds as chemotherapeutic agents.

Four new natural and two semisynthetic 15,24,30-trioxygenated acetogenins were tested as mitochondrial complex I enzymatic inhibitors as well as growth of several tumor cell lines. Placement of acetyl groups along the alkyl chain modulated the potency of the bis-tetrahydrofuranic acetogenins.Figure optionsDownload as PowerPoint slide